subject:(Imidazo 1 2 a pyridine)

1. Tber, Zahira. L'imidazo[1,2-a]pyridine : fonctionnalisation et synthèse des nouveaux polyhétérocycles : Imidazo[1,2-a]pyridine : functionalization and synthesis of new polyheterocycles.

Degree: Docteur es, Chimie organique, 2016, Orléans; Université Hassan II (Casablanca, Maroc)

URL: http://www.theses.fr/2016ORLE2021

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Les préparations de composés comportant un noyau imidazo[1,2-a]pyridinique constituent un thème de recherche important en synthèse organique, compte tenu des nombreuses activités biologiques qu’ils peuvent… (more)

Subjects/Keywords: Imidazo[1,2-a]pyridine; Catalyse; Cuivre; Fer; Thioethers; Réaction multicomposants; Pyrrolo[3',2':4,5]imidazo[1,2-a]pyridines; 5-aminopyrido[2’,1’:2,3]imidazo[4,5-c]isoquinoléines; Imidazo[1,2-a]pyridine; Catalyst; Copper; Iron; Thioethes; Multicomponent reaction; Pyrrolo[3',2':4,5]imidazo[1,2-a]pyridines; 5-aminopyrido[2’,1’:2,3]imidazo[4,5-c]isoquinolines; 547.59

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Tber, Z. (2016). L'imidazo[1,2-a]pyridine : fonctionnalisation et synthèse des nouveaux polyhétérocycles : Imidazo[1,2-a]pyridine : functionalization and synthesis of new polyheterocycles. (Doctoral Dissertation). Orléans; Université Hassan II (Casablanca, Maroc). Retrieved from http://www.theses.fr/2016ORLE2021

Chicago Manual of Style (16^th Edition):

Tber, Zahira. “L'imidazo[1,2-a]pyridine : fonctionnalisation et synthèse des nouveaux polyhétérocycles : Imidazo[1,2-a]pyridine : functionalization and synthesis of new polyheterocycles.” 2016. Doctoral Dissertation, Orléans; Université Hassan II (Casablanca, Maroc). Accessed January 26, 2021. http://www.theses.fr/2016ORLE2021.

MLA Handbook (7^th Edition):

Tber, Zahira. “L'imidazo[1,2-a]pyridine : fonctionnalisation et synthèse des nouveaux polyhétérocycles : Imidazo[1,2-a]pyridine : functionalization and synthesis of new polyheterocycles.” 2016. Web. 26 Jan 2021.

Vancouver:

Tber Z. L'imidazo[1,2-a]pyridine : fonctionnalisation et synthèse des nouveaux polyhétérocycles : Imidazo[1,2-a]pyridine : functionalization and synthesis of new polyheterocycles. [Internet] [Doctoral dissertation]. Orléans; Université Hassan II (Casablanca, Maroc); 2016. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2016ORLE2021.

Council of Science Editors:

Tber Z. L'imidazo[1,2-a]pyridine : fonctionnalisation et synthèse des nouveaux polyhétérocycles : Imidazo[1,2-a]pyridine : functionalization and synthesis of new polyheterocycles. [Doctoral Dissertation]. Orléans; Université Hassan II (Casablanca, Maroc); 2016. Available from: http://www.theses.fr/2016ORLE2021

2. Fersing, Cyril. Synthèse et étude des relations structure-activité de nouvelles 3-nitroimidazo (1,2-a) pyridines anti-kinétoplastidés : Synthesis and structure-activity relationships study of new anti-kinetoplastid 3-nitroimidazo[1,2-a]pyridines.

Degree: Docteur es, Sciences Chimiques, 2018, Aix Marseille Université

URL: http://www.theses.fr/2018AIXM0275

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Les maladies tropicales négligées causées par les protozoaires kinétoplastidés du genre Leishmania et Trypanosoma représentent une menace pour près d’un demi-milliard de personnes en zone… (more)

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Les maladies tropicales négligées causées par les protozoaires kinétoplastidés du genre Leishmania et Trypanosoma représentent une menace pour près d’un demi-milliard de personnes en zone intertropicale, entrainant jusqu’à 50 000 décès par an. Parmi les molécules en développement clinique pour traiter ces pathologies, le fexinidazole est une prodrogue appartenant à la famille des 5-nitroimidazoles et qui exerce son action anti-infectieuse via une étape de bioactivation catalysée par des nitroréductases (NTR) parasitaires, enzymes dont le co-facteur est une flavine. Afin d’identifier de nouveaux nitrohétérocycles antiparasitaires substrats des NTR, une petite chimiothèque d’imidazo[1,2-a]pyridines synthétisées au laboratoire a subi un criblage in vitro ayant conduit à l’identification d’une molécule Hit, à la fois active sur Leishmania donovani et Trypanosoma brucei brucei. Ce composé a servi de point de départ à un travail de pharmacomodulation, dans un premier temps en position 8 du cycle imidazo[1,2-a]pyridine : l’introduction de groupements variés à l’aide de réactions de couplage pallado-catalysées de Suzuki-Miyaura, Sonogashira et Buchwald-Hartwig ou des réactions de SNAr, a permis de mettre en lumière plusieurs composés « tête de série » au profil biologique nettement amélioré. Dans un second temps, le travail de pharmacomodulation entrepris a été étendu aux positions 2, 3 et 6 du cycle imidazo[1,2-a]pyridine en vue de compléter les données de relations structure-activité, d’étudier en particulier l’impact du potentiel rédox et d’optimiser les paramètres physico-chimiques et pharmacocinétiques in vitro des meilleurs composés.

The kinetoplastids of the Leishmania and Trypanosoma genus are the causative agents of neglected tropical diseases that threaten nearly half a billion people in the intertropical zone, resulting in 50 000 deaths per year. Among the molecules in clinical development to treat these pathologies, fexinidazole is a prodrug belonging to the 5-nitroimidazoles family, which exerts its anti-infectious action via a bioactivation step catalyzed by parasitic nitroreductases (NTR), enzymes whose cofactor is a flavin. In order to identify novel nitroheterocycles as parasitic NTR substrates, a small chemical library of imidazo[1,2-a]pyridines synthesized by our laboratory was screened in vitro, leading to the identification of a Hit molecule active both on Leishmania donovani and Trypanosoma brucei brucei. This compound served as a starting point for a pharmacomodulation work, initially in position 8 of the imidazo[1,2-a]pyridine ring: the introduction of various chemical groups using the pallado-catalyzed coupling reactions of Suzuki-Miyaura, Sonogashira and Buchwald-Hartwig, or SNAr reactions, highlighted several "lead" compounds with a significantly improved biological profile. In a second step, the pharmacomodulation work was extended to positions 2, 3 and 6 of the imidazo[1,2-a]pyridine ring in order to complete the structure-activity relationship data, to study in particular the impact of the…

Advisors/Committee Members: Rathelot, Pascal (thesis director), Verhaeghe, Pierre (thesis director).

Subjects/Keywords: Pharmacomodulation anti-Kinétoplastidés; Nitrohétérocycles; Nitroréductases; Couplages pallado-Catalysés; Relations structure-Activité; Leishmania sp; Trypanosoma sp.; Imidazo[1; 2-A]pyridine; Anti-Kinetoplastids pharmacomodulation; Nitroheterocycles; Nitroreductases; Imidazo[1; 2-A]pyridine; Palladium-Catalyzed cross-Coupling reactions; Structure-Activity relationships; Leishmania spp; Trypanosoma spp.; Imidazo[1; 2-A]pyridine

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Fersing, C. (2018). Synthèse et étude des relations structure-activité de nouvelles 3-nitroimidazo (1,2-a) pyridines anti-kinétoplastidés : Synthesis and structure-activity relationships study of new anti-kinetoplastid 3-nitroimidazo[1,2-a]pyridines. (Doctoral Dissertation). Aix Marseille Université. Retrieved from http://www.theses.fr/2018AIXM0275

Chicago Manual of Style (16^th Edition):

Fersing, Cyril. “Synthèse et étude des relations structure-activité de nouvelles 3-nitroimidazo (1,2-a) pyridines anti-kinétoplastidés : Synthesis and structure-activity relationships study of new anti-kinetoplastid 3-nitroimidazo[1,2-a]pyridines.” 2018. Doctoral Dissertation, Aix Marseille Université. Accessed January 26, 2021. http://www.theses.fr/2018AIXM0275.

MLA Handbook (7^th Edition):

Fersing, Cyril. “Synthèse et étude des relations structure-activité de nouvelles 3-nitroimidazo (1,2-a) pyridines anti-kinétoplastidés : Synthesis and structure-activity relationships study of new anti-kinetoplastid 3-nitroimidazo[1,2-a]pyridines.” 2018. Web. 26 Jan 2021.

Vancouver:

Fersing C. Synthèse et étude des relations structure-activité de nouvelles 3-nitroimidazo (1,2-a) pyridines anti-kinétoplastidés : Synthesis and structure-activity relationships study of new anti-kinetoplastid 3-nitroimidazo[1,2-a]pyridines. [Internet] [Doctoral dissertation]. Aix Marseille Université 2018. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2018AIXM0275.

Council of Science Editors:

Fersing C. Synthèse et étude des relations structure-activité de nouvelles 3-nitroimidazo (1,2-a) pyridines anti-kinétoplastidés : Synthesis and structure-activity relationships study of new anti-kinetoplastid 3-nitroimidazo[1,2-a]pyridines. [Doctoral Dissertation]. Aix Marseille Université 2018. Available from: http://www.theses.fr/2018AIXM0275

NSYSU

3. Chen, Wun-Yu. Hypervalent Iodine-Mediated Reaction of Anilines with Pyridines to Benzo[4,5]imidazo[1,2-a]pyridine Derivatives.

Degree: Master, Chemistry, 2017, NSYSU

URL: http://etd.lib.nsysu.edu.tw/ETD-db/ETD-search/view_etd?URN=etd-0619117-144154

► It was found that hypervalent iodine, such as (diacetoxyiodo)benzene and [bis(trifluoroacetoxy)iodo]benzene could mediate reaction of anilines with pyridines in mild reaction to give benzo[4,5]imidazo[1,2-a]pyridine derivatives.… (more)

Subjects/Keywords: nitrenium ion; 2-a]pyridine; heterocycles compound; cation radical; benzo[4; 5]imidazo[1; benzimidazole; hypervalent iodine

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Chen, W. (2017). Hypervalent Iodine-Mediated Reaction of Anilines with Pyridines to Benzo[4,5]imidazo[1,2-a]pyridine Derivatives. (Thesis). NSYSU. Retrieved from http://etd.lib.nsysu.edu.tw/ETD-db/ETD-search/view_etd?URN=etd-0619117-144154

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Chen, Wun-Yu. “Hypervalent Iodine-Mediated Reaction of Anilines with Pyridines to Benzo[4,5]imidazo[1,2-a]pyridine Derivatives.” 2017. Thesis, NSYSU. Accessed January 26, 2021. http://etd.lib.nsysu.edu.tw/ETD-db/ETD-search/view_etd?URN=etd-0619117-144154.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Chen, Wun-Yu. “Hypervalent Iodine-Mediated Reaction of Anilines with Pyridines to Benzo[4,5]imidazo[1,2-a]pyridine Derivatives.” 2017. Web. 26 Jan 2021.

Vancouver:

Chen W. Hypervalent Iodine-Mediated Reaction of Anilines with Pyridines to Benzo[4,5]imidazo[1,2-a]pyridine Derivatives. [Internet] [Thesis]. NSYSU; 2017. [cited 2021 Jan 26]. Available from: http://etd.lib.nsysu.edu.tw/ETD-db/ETD-search/view_etd?URN=etd-0619117-144154.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Chen W. Hypervalent Iodine-Mediated Reaction of Anilines with Pyridines to Benzo[4,5]imidazo[1,2-a]pyridine Derivatives. [Thesis]. NSYSU; 2017. Available from: http://etd.lib.nsysu.edu.tw/ETD-db/ETD-search/view_etd?URN=etd-0619117-144154

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

4. Juillet, Charlotte. Conception, synthèse et évaluation pharmacologique d’analogues simplifiés de métabolites marins, inhibiteurs de la kinase Aurora B, à visée anticancéreuse : Conception, synthesis and biological evaluation of simplified analogs from marine metabolites as Aurora B kinase inhibitors for cancer therapy.

Degree: Docteur es, Chimie, 2020, université Paris-Saclay

URL: http://www.theses.fr/2020UPASF019

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Ce manuscrit porte sur la conception, la synthèse et l’évaluation biologique d’analogues de l’oroïdine, monomère de la benzosceptrine C. Ces molécules sont issues de la… (more)

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Ce manuscrit porte sur la conception, la synthèse et l’évaluation biologique d’analogues de l’oroïdine, monomère de la benzosceptrine C. Ces molécules sont issues de la famille des pyrrole-2-aminoimidazoles, isolées d’éponges marines. La stratégie de simplification et de diversification structurale a conduit à l’identification d’un hit sélectif, inhibiteur de la kinase Aurora B. Celle-ci joue un rôle essentiel dans la division cellulaire et son inhibition conduit à des anomalies mitotiques sévères. De plus, elle est surexprimée dans de nombreux cancers, en faisant une cible thérapeutique de choix en oncologie. L’objectif du projet, à l’interface entre la chimie et la biologie, était de synthétiser un composé chef de file pouvant conduire à un candidat médicament à visée anticancéreuse. Le squelette du hit est constitué de trois parties : une partie 4,5-dibromopyrrole, une partie imidazo[1,2-a]pyrimidine et enfin un linker alcyne. Le travail de chimie médicinal s’est articulé autour de ces trois sites de modulation structurale, qui ont été successivement modifiés et font l’objet des chapitres II à IV, après le chapitre I dédié à l’introduction. Finalement, quatre-vingt deux dérivés ont été synthétisés et évalués in vitro sur Aurora B et un panel de kinases impliquées dans différentes pathologies. Plusieurs analogues se sont avérés très actifs, avec des IC50 allant jusqu’à 34 nM, soit 150 fois plus actifs que le hit initial. Le dernier chapitre porte sur l’étude du mode d’action des inhibiteurs les plus actifs. Des études de cinétiques enzymatiques ont mis en évidence un mode d’inhibition non-ATP compétitif, jusqu’alors jamais décrit pour Aurora B. Par ailleurs, des expériences d’immunomarquage ont permis d’évaluer et de quantifier les effets du meilleur composé sur les cellules traitées, montrant des résultats cohérents avec l’inhibition d’Aurora B. Enfin, des études de modélisation moléculaire avec le meilleur inhibiteur nous ont permis de situer le site de fixation potentiel de nos inhibiteurs afin de poursuivre les pharmacomodulations et l’étude SAR. Le manuscript se termine par une conclusion générale et des perspectives qui proposent des pistes pour optimiser les propriétés physicochimiques et pharmacocinétiques afin d’améliorer les propriétés nécessaires à un candidat médicament.

This manuscript describes the design, synthesis and biological evaluation of oroidin analogs. Oroidin is a monomer of benzosceptrin C, belonging to the pyrrole-2-aminoimidazole family, isolated from marine sponges. The simplification and structural diversification approaches led us to the identification of a non-natural hit displaying selective inhibitory activity against the kinase Aurora B. This kinase plays a key role in cell division and its inhibition leads to severe mitotic abnormalities. Aurora B is found to be up-regulated in many human cancers, indicating that this kinase is a cancer-relevant target. The objective of the study at the interface between chemistry and biology is to optimize the discovered hit into a lead. The…

Advisors/Committee Members: Al-Mourabit, Ali (thesis director).

Subjects/Keywords: Chimie médicinale; Métabolites marins; Imidazo[1,2-a]pyridine; Inhibiteurs de kinases; Cancer; Aurora; Medicinal chemistry; Marine metabolites; Imidazo[1,2-a]pyridine; Kinase inhibitors; Cancer; Aurora

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Juillet, C. (2020). Conception, synthèse et évaluation pharmacologique d’analogues simplifiés de métabolites marins, inhibiteurs de la kinase Aurora B, à visée anticancéreuse : Conception, synthesis and biological evaluation of simplified analogs from marine metabolites as Aurora B kinase inhibitors for cancer therapy. (Doctoral Dissertation). université Paris-Saclay. Retrieved from http://www.theses.fr/2020UPASF019

Chicago Manual of Style (16^th Edition):

Juillet, Charlotte. “Conception, synthèse et évaluation pharmacologique d’analogues simplifiés de métabolites marins, inhibiteurs de la kinase Aurora B, à visée anticancéreuse : Conception, synthesis and biological evaluation of simplified analogs from marine metabolites as Aurora B kinase inhibitors for cancer therapy.” 2020. Doctoral Dissertation, université Paris-Saclay. Accessed January 26, 2021. http://www.theses.fr/2020UPASF019.

MLA Handbook (7^th Edition):

Juillet, Charlotte. “Conception, synthèse et évaluation pharmacologique d’analogues simplifiés de métabolites marins, inhibiteurs de la kinase Aurora B, à visée anticancéreuse : Conception, synthesis and biological evaluation of simplified analogs from marine metabolites as Aurora B kinase inhibitors for cancer therapy.” 2020. Web. 26 Jan 2021.

Vancouver:

Juillet C. Conception, synthèse et évaluation pharmacologique d’analogues simplifiés de métabolites marins, inhibiteurs de la kinase Aurora B, à visée anticancéreuse : Conception, synthesis and biological evaluation of simplified analogs from marine metabolites as Aurora B kinase inhibitors for cancer therapy. [Internet] [Doctoral dissertation]. université Paris-Saclay; 2020. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2020UPASF019.

Council of Science Editors:

Juillet C. Conception, synthèse et évaluation pharmacologique d’analogues simplifiés de métabolites marins, inhibiteurs de la kinase Aurora B, à visée anticancéreuse : Conception, synthesis and biological evaluation of simplified analogs from marine metabolites as Aurora B kinase inhibitors for cancer therapy. [Doctoral Dissertation]. université Paris-Saclay; 2020. Available from: http://www.theses.fr/2020UPASF019

Vilnius University

5. Juškėnas, Robertas. Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals.

Degree: PhD, Chemistry, 2014, Vilnius University

URL: http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154044-28576 ;

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The development of heterocyclic chemistry is important for various science areas and for the industry. The main task of this branch of chemistry is the… (more)

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The development of heterocyclic chemistry is important for various science areas and for the industry. The main task of this branch of chemistry is the search for the new, more effective synthetic methods for obtaining heterocyclic derivatives. That covers not only the formation of heterocycles, but also their functionalization, which leads to the creation of compounds having various chemical and physical properties. The accomplishments of this area are applied in biochemistry, pharmacochemistry, photophysics and other branches of science and industry. The creation of effective heterocycles synthesis methods, that may be applied for the formation of heterosystems based on pyrazolo[3,4-d]pyrimidine was the main aim in this work. During this work, three hitherto unknown peri-fused heterocyclic systems based on pyrazolo[3,4-d]pyrimidine scaffold were synthesized. The suitable conditions for the cyclization of 4-(2,2-diethoxyethyl)aminopyrimidines to 2,3-dihydroimidazo[1,2-c]pyrimidines were found. The influence of functional groups in pyrimidine moiety for the course of this reaction was investigated. It has been shown that functional groups including alkylthio, cyano, amino, formyl are tolerated in this type of reaction. The method for the replacement of ethoxy group with benzyl mercaptan in 3-ethoxy-2,3-dihydroimidazo[1,2-c]pyrazolo[4,3-e]pyrimidines has been found.

Heterociklų chemijos vystymasis turi didelę reikšmę įvairioms mokslo sritims ir pramonės raidai. Pagrindinis šios chemijos srities uždavinys – kurti naujus heterociklinių junginių sintezės metodus, leidžiančius paprasčiau, efektyviau gauti norimos struktūros junginius. Tai apima ne tik heterociklų formavimo būdus, bet ir jų funkcionalizavimą, leidžiantį sukurti įvairiomis cheminėmis ir fizikinėmis savybėmis pasižyminčių junginių įvairovę. Šios mokslo srities pasiekimai pritaikomi biochemijoje, farmacijoje, fotofizikoje ir kitose mokslo ir pramonės šakose. Šiame darbe buvo siekiama sukurti efektyvius heterosistemų sintezės būdus, kuriuos galima pritaikyti pirazolo[3,4-d]pirimidino fragmentą turinčių heterociklų formavimui. Šio darbo metu buvo susintetintos trys iki šiol neaprašytos heterociklinės sistemos atliekant peri-kondensuotų heterosistemų sintezę iš 3-amino-4-chlor-1-metil-6-metiltio-1H-pirazolo[3,4-d]pirimidino. Surastos tinkamos sąlygos 4-(2,2-dietoksietilmino)pirimidinų ciklizacijai į 3-etoksi-2,3-dihidroimidazo[1,2-c]pirimidinus. Ištirta pirimidino žiede esančių pakaitų įtaka šiai reakcijai. Parodyta, kad ši reakcija yra suderinama su tokiomis funkcinėmis grupėmis, kaip alkiltio-, cian-, amino-, formilgrupės. Surastas metodas 3-etoksi-2,3-dihidroimidazo[1,2-c]pirazolo[4,3-e]pirimidinų etoksigrupės pakeitimui benziltiogrupe.

Advisors/Committee Members: BUTKUS, EUGENIJUS (Doctoral dissertation committee chair), BERESNEVIČIUS, ZIGMUNDAS JONAS (Doctoral dissertation committee member), DODONOVA, JELENA (Doctoral dissertation committee member), MALINAUSKAS, ALBERTAS (Doctoral dissertation committee member), MICKEVIČIUS, VYTAUTAS (Doctoral dissertation committee member), JAKUBKIENĖ, VIRGINIJA (Doctoral dissertation opponent), GETAUTIS, VYTAUTAS (Doctoral dissertation opponent), MASEVIČIUS, VIKTORAS (Doctoral dissertation supervisor).

Subjects/Keywords: Heterocycles; Cyclization; Acetals; Imidazo[1; 2-c]pyrimidines; Heterociklai; Ciklizacija; Acetaliai; Imidazo[1; 2-c]pirimidinai

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Juškėnas, R. (2014). Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals. (Doctoral Dissertation). Vilnius University. Retrieved from http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154044-28576 ;

Chicago Manual of Style (16^th Edition):

Juškėnas, Robertas. “Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals.” 2014. Doctoral Dissertation, Vilnius University. Accessed January 26, 2021. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154044-28576 ;.

MLA Handbook (7^th Edition):

Juškėnas, Robertas. “Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals.” 2014. Web. 26 Jan 2021.

Vancouver:

Juškėnas R. Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals. [Internet] [Doctoral dissertation]. Vilnius University; 2014. [cited 2021 Jan 26]. Available from: http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154044-28576 ;.

Council of Science Editors:

Juškėnas R. Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals. [Doctoral Dissertation]. Vilnius University; 2014. Available from: http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154044-28576 ;

Vilnius University

6. Juškėnas, Robertas. Triciklių heterosistemų, turinčių pirazolo[3,4-d]pirimidino fragmentą, sintezė. Intramolekulinės pirimidino azoto atomo reakcijos su O,O-acetaliais tyrimas.

Degree: Dissertation, Chemistry, 2014, Vilnius University

URL: http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154058-49723 ;

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Heterociklų chemijos vystymasis turi didelę reikšmę įvairioms mokslo sritims ir pramonės raidai. Pagrindinis šios chemijos srities uždavinys – kurti naujus heterociklinių junginių sintezės metodus, leidžiančius… (more)

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Heterociklų chemijos vystymasis turi didelę reikšmę įvairioms mokslo sritims ir pramonės raidai. Pagrindinis šios chemijos srities uždavinys – kurti naujus heterociklinių junginių sintezės metodus, leidžiančius paprasčiau, efektyviau gauti norimos struktūros junginius. Tai apima ne tik heterociklų formavimo būdus, bet ir jų funkcionalizavimą, leidžiantį sukurti įvairiomis cheminėmis ir fizikinėmis savybėmis pasižyminčių junginių įvairovę. Šios mokslo srities pasiekimai pritaikomi biochemijoje, farmacijoje, fotofizikoje ir kitose mokslo ir pramonės šakose. Šiame darbe buvo siekiama sukurti efektyvius heterosistemų sintezės būdus, kuriuos galima pritaikyti pirazolo[3,4-d]pirimidino fragmentą turinčių heterociklų formavimui. Šio darbo metu buvo susintetintos trys iki šiol neaprašytos heterociklinės sistemos atliekant peri-kondensuotų heterosistemų sintezę iš 3-amino-4-chlor-1-metil-6-metiltio-1H-pirazolo[3,4-d]pirimidino. Surastos tinkamos sąlygos 4-(2,2-dietoksietilmino)pirimidinų ciklizacijai į 3-etoksi-2,3-dihidroimidazo[1,2-c]pirimidinus. Ištirta pirimidino žiede esančių pakaitų įtaka šiai reakcijai. Parodyta, kad ši reakcija yra suderinama su tokiomis funkcinėmis grupėmis, kaip alkiltio-, cian-, amino-, formilgrupės. Surastas metodas 3-etoksi-2,3-dihidroimidazo[1,2-c]pirazolo[4,3-e]pirimidinų etoksigrupės pakeitimui benziltiogrupe.

The development of heterocyclic chemistry is important for various science areas and for the industry. The main task of this branch of chemistry is the search for the new, more effective synthetic methods for obtaining heterocyclic derivatives. That covers not only the formation of heterocycles, but also their functionalization, which leads to the creation of compounds having various chemical and physical properties. The accomplishments of this area are applied in biochemistry, pharmacochemistry, photophysics and other branches of science and industry. The creation of effective heterocycles synthesis methods, that may be applied for the formation of heterosystems based on pyrazolo[3,4-d]pyrimidine was the main aim in this work. During this work, three hitherto unknown peri-fused heterocyclic systems based on pyrazolo[3,4-d]pyrimidine scaffold were synthesized. The suitable conditions for the cyclization of 4-(2,2-diethoxyethyl)aminopyrimidines to 2,3-dihydroimidazo[1,2-c]pyrimidines were found. The influence of functional groups in pyrimidine moiety for the course of this reaction was investigated. It has been shown that functional groups including alkylthio, cyano, amino, formyl are tolerated in this type of reaction. The method for the replacement of ethoxy group with benzyl mercaptan in 3-ethoxy-2,3-dihydroimidazo[1,2-c]pyrazolo[4,3-e]pyrimidines has been found.

Advisors/Committee Members: BUTKUS, EUGENIJUS (Doctoral dissertation committee chair), BERESNEVIČIUS, ZIGMUNDAS JONAS (Doctoral dissertation committee member), DODONOVA, JELENA (Doctoral dissertation committee member), MALINAUSKAS, ALBERTAS (Doctoral dissertation committee member), MICKEVIČIUS, VYTAUTAS (Doctoral dissertation committee member), JAKUBKIENĖ, VIRGINIJA (Doctoral dissertation opponent), GETAUTIS, VYTAUTAS (Doctoral dissertation opponent), MASEVIČIUS, VIKTORAS (Doctoral dissertation supervisor).

Subjects/Keywords: Heterociklai; Ciklizacija; Acetaliai; Imidazo[1; 2-c]pirimidinai; Heterocycles; Cyclization; Acetals; Imidazo[1; 2-c]pyrimidines

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APA (6^th Edition):

Juškėnas, R. (2014). Triciklių heterosistemų, turinčių pirazolo[3,4-d]pirimidino fragmentą, sintezė. Intramolekulinės pirimidino azoto atomo reakcijos su O,O-acetaliais tyrimas. (Doctoral Dissertation). Vilnius University. Retrieved from http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154058-49723 ;

Chicago Manual of Style (16^th Edition):

Juškėnas, Robertas. “Triciklių heterosistemų, turinčių pirazolo[3,4-d]pirimidino fragmentą, sintezė. Intramolekulinės pirimidino azoto atomo reakcijos su O,O-acetaliais tyrimas.” 2014. Doctoral Dissertation, Vilnius University. Accessed January 26, 2021. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154058-49723 ;.

MLA Handbook (7^th Edition):

Juškėnas, Robertas. “Triciklių heterosistemų, turinčių pirazolo[3,4-d]pirimidino fragmentą, sintezė. Intramolekulinės pirimidino azoto atomo reakcijos su O,O-acetaliais tyrimas.” 2014. Web. 26 Jan 2021.

Vancouver:

Juškėnas R. Triciklių heterosistemų, turinčių pirazolo[3,4-d]pirimidino fragmentą, sintezė. Intramolekulinės pirimidino azoto atomo reakcijos su O,O-acetaliais tyrimas. [Internet] [Doctoral dissertation]. Vilnius University; 2014. [cited 2021 Jan 26]. Available from: http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154058-49723 ;.

Council of Science Editors:

Juškėnas R. Triciklių heterosistemų, turinčių pirazolo[3,4-d]pirimidino fragmentą, sintezė. Intramolekulinės pirimidino azoto atomo reakcijos su O,O-acetaliais tyrimas. [Doctoral Dissertation]. Vilnius University; 2014. Available from: http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154058-49723 ;

Univerzitet u Beogradu

7. Petković, Miloš R., 1980-. Reakcije alena i nukleofila katalizovane paladijumovim kompleksima.

Degree: Hemijski fakultet, 2016, Univerzitet u Beogradu

URL: https://fedorabg.bg.ac.rs/fedora/get/o:12522/bdef:Content/get

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Hemija - Organska hemija / Chemistry - Organic chemistry

U sklopu ove doktorske teze proučavane su transformacije alena u prisustvu paladijumovih kompleksa, a posebno reaktivnost… (more)

Subjects/Keywords: allenes; π-allylpalladium; allyl acetates; imidazo[1; 2-a]pyridine; synthesis; isomerization; cyclization

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APA (6^th Edition):

Petković, Miloš R., 1. (2016). Reakcije alena i nukleofila katalizovane paladijumovim kompleksima. (Thesis). Univerzitet u Beogradu. Retrieved from https://fedorabg.bg.ac.rs/fedora/get/o:12522/bdef:Content/get

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Petković, Miloš R., 1980-. “Reakcije alena i nukleofila katalizovane paladijumovim kompleksima.” 2016. Thesis, Univerzitet u Beogradu. Accessed January 26, 2021. https://fedorabg.bg.ac.rs/fedora/get/o:12522/bdef:Content/get.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Petković, Miloš R., 1980-. “Reakcije alena i nukleofila katalizovane paladijumovim kompleksima.” 2016. Web. 26 Jan 2021.

Vancouver:

Petković, Miloš R. 1. Reakcije alena i nukleofila katalizovane paladijumovim kompleksima. [Internet] [Thesis]. Univerzitet u Beogradu; 2016. [cited 2021 Jan 26]. Available from: https://fedorabg.bg.ac.rs/fedora/get/o:12522/bdef:Content/get.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Petković, Miloš R. 1. Reakcije alena i nukleofila katalizovane paladijumovim kompleksima. [Thesis]. Univerzitet u Beogradu; 2016. Available from: https://fedorabg.bg.ac.rs/fedora/get/o:12522/bdef:Content/get

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of Michigan

8. Williams, John David. Design, synthesis, and antiviral activity of TCRB analogs based on imidazo[1,2-a]pyridine, pyrazolo[1,5-a]pyridine, and indole heterocycles.

Degree: PhD, Pure Sciences, 2003, University of Michigan

URL: http://hdl.handle.net/2027.42/123978

► Human cytomegalovirus (HCMV) is an opportunistic virus which causes serious pathologies in immunocompromised populations. Although several drugs have been approved for the treatment of HCMV-related… (more)

Subjects/Keywords: Activity; Analogs; Antiviral; Based; Design; Heterocycles; Imidazo[1,2-a]pyridine; Indole; Pyrazolo[1,5-a]pyridine; Synthesis; Tcrb; Trichloro-1-(beta-d-ribofuranosyl)benzimidazole-2,5,6

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Williams, J. D. (2003). Design, synthesis, and antiviral activity of TCRB analogs based on imidazo[1,2-a]pyridine, pyrazolo[1,5-a]pyridine, and indole heterocycles. (Doctoral Dissertation). University of Michigan. Retrieved from http://hdl.handle.net/2027.42/123978

Chicago Manual of Style (16^th Edition):

Williams, John David. “Design, synthesis, and antiviral activity of TCRB analogs based on imidazo[1,2-a]pyridine, pyrazolo[1,5-a]pyridine, and indole heterocycles.” 2003. Doctoral Dissertation, University of Michigan. Accessed January 26, 2021. http://hdl.handle.net/2027.42/123978.

MLA Handbook (7^th Edition):

Williams, John David. “Design, synthesis, and antiviral activity of TCRB analogs based on imidazo[1,2-a]pyridine, pyrazolo[1,5-a]pyridine, and indole heterocycles.” 2003. Web. 26 Jan 2021.

Vancouver:

Williams JD. Design, synthesis, and antiviral activity of TCRB analogs based on imidazo[1,2-a]pyridine, pyrazolo[1,5-a]pyridine, and indole heterocycles. [Internet] [Doctoral dissertation]. University of Michigan; 2003. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/2027.42/123978.

Council of Science Editors:

Williams JD. Design, synthesis, and antiviral activity of TCRB analogs based on imidazo[1,2-a]pyridine, pyrazolo[1,5-a]pyridine, and indole heterocycles. [Doctoral Dissertation]. University of Michigan; 2003. Available from: http://hdl.handle.net/2027.42/123978

9. Zhang, Jianbo. Impact of Gut Microbiota on the Metabolism of Carcinogenic Dietary Heterocyclic Amines.

Degree: 2018, ETH Zürich

URL: http://hdl.handle.net/20.500.11850/280012

► Human are constantly exposed to potentially toxic chemicals from the environment, diet, and therapeutic interventions. However, the gut harbors a diverse community of microorganisms, which… (more)

▼ Human are constantly exposed to potentially toxic chemicals from the environment, diet, and therapeutic interventions. However, the gut harbors a diverse community of microorganisms, which may alter the exposure and toxicity of these chemicals. Heterocyclic amines (HCAs) are mutagens presented in meat cooked at high temperature, and they are strongly associated with the increased risk of colorectal cancer. Bacterial transformation of HCAs may alter their structures and thus their toxicity, but little is known regarding the influence of gut microbiota on the risk associated with these chemicals due to the existing knowledge gap regarding the microbiota-chemical interactions. The work described in this thesis concerns the chemical and biochemical mechanisms of commensal gut bacterial transformation of HCAs and their liver metabolites, as well as toxicological and physiological relevance of the microbial transformations. The knowledge obtained provides mechanistic insights on how gut microbiota alter chemical toxicity and supports gut microbiota as a factor in the risk assessment of toxic chemicals. Chapter 1 introduces the background information concerning the microbial metabolism of glycerol in the human gut and its relevance to HCA transformation. In addition, an overview of the potential targets of gut bacteria-derived acrolein is given. In Chapter 2, we aimed to address the generality of bacterial conjugation of HCAs with acrolein. MeIQx is an imidazoquinoxaline mutagen ten times more mutagenic than PhIP toward bacterial DNA in vitro assays. E. hallii, Lactobacillus reuteri, and Lactobacillus rossiae were found to convert MeIQx to a new microbial metabolite characterized on the basis of HRMS and NMR as 9-hydroxyl-2,7-dimethyl-7,9,10,11-tetrahydropyrimido-[2′,1′:2,3]imidazo[4,5-f]quinoxaline (MeIQx-M1). Acrolein derived from the decomposition of 3-HPA, which is a product of glycerol reduction mediated by GDH activity, was identified as the active compound responsible for the formation of MeIQx-M1. MeIQx-M1 appears to have slightly reduced cytotoxic potency toward human colon epithelial cells, and diminished mutagenic potential toward bacteria after metabolic activation. In Chapter 3, the physiological and toxicological relevance of the microbial transformation of MeIQx to MeIQx-M1 was characterized. To address whether the microbial transformation influences the intestinal transport of MeIQx, the intestinal uptake of MeIQx and its metabolite MeIQx-M1 was quantified with ex vivo rat intestinal segments, however, only negligible amounts of both MeIQx and MeIQx-M1 were transported. In addition, neither MeIQx nor MeIQx-M1 were cytotoxic towards liver HepaRG cells at dietary levels or higher concentrations. Physiologically based pharmacokinetic modeling suggests that increased microbial transformation of MeIQx can reduce plasma levels of MeIQx, potentially contributing to reduced systemic exposure of MeIQx in human. In Chapter 4, the impact of commensal gut microbes on the transformation of HCA liver metabolites,… Advisors/Committee Members: Sturla, Shana J., id_orcid0000-0001-6808-5950, Lacroix, Christophe, id_orcid0000-0003-4360-2020, Steinberg, Pablo, Schwab, Clarissa.

Subjects/Keywords: acrolein; Gut microbiota; Biotransformation; 9-hydroxyl-2,7-dimethyl-7,9,10,11-tetrahydropyrimido-[2′,1′:2,3]imidazo[4,5-f]quinoxaline; Eubacterium hallii; 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine; Glycerol/diol dehydratase; Reuterin; Heterocyclic amine; MeIQx-M1; Food carcinogen; Detoxification; Lactobacillus reuteri; info:eu-repo/classification/ddc/610; info:eu-repo/classification/ddc/570; Medical sciences, medicine; Life sciences

10 more images…

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Zhang, J. (2018). Impact of Gut Microbiota on the Metabolism of Carcinogenic Dietary Heterocyclic Amines. (Doctoral Dissertation). ETH Zürich. Retrieved from http://hdl.handle.net/20.500.11850/280012

Chicago Manual of Style (16^th Edition):

Zhang, Jianbo. “Impact of Gut Microbiota on the Metabolism of Carcinogenic Dietary Heterocyclic Amines.” 2018. Doctoral Dissertation, ETH Zürich. Accessed January 26, 2021. http://hdl.handle.net/20.500.11850/280012.

MLA Handbook (7^th Edition):

Zhang, Jianbo. “Impact of Gut Microbiota on the Metabolism of Carcinogenic Dietary Heterocyclic Amines.” 2018. Web. 26 Jan 2021.

Vancouver:

Zhang J. Impact of Gut Microbiota on the Metabolism of Carcinogenic Dietary Heterocyclic Amines. [Internet] [Doctoral dissertation]. ETH Zürich; 2018. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/20.500.11850/280012.

Council of Science Editors:

Zhang J. Impact of Gut Microbiota on the Metabolism of Carcinogenic Dietary Heterocyclic Amines. [Doctoral Dissertation]. ETH Zürich; 2018. Available from: http://hdl.handle.net/20.500.11850/280012

10. Grosse, Sandrine. Imidazo[1, 2-b]pyrazoles, imidazo[1, 2-a]imidazoles : synthèse, fonctionnalisation et évaluation biologique : Imidazo[1,2-b]pyrazoles, imidazo[1,2-a]imidazoles : synthesis, functionalisation and biological evaluation.

Degree: Docteur es, Chimie organique, 2013, Université d'Orléans

URL: http://www.theses.fr/2013ORLE2056

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Les imidazo[1,2-b]pyrazoles tout comme les imidazo[1,2-a]imidazoles sont des entités présentant diverses applications intéressantes notamment dans le domaine pharmacologique. Cependant, malgré ce potentiel, ces structures hétérobicycliques… (more)

Subjects/Keywords: Imidazo[1,2-b]pyrazoles; Imidazo[1,2-a]imidazoles; Imidazo[1,2-a]imidazolin-2-ones; (hétéro)arylation directe; Metallo-catalysées; Régioselectivité; Suzuki-Miyaura; Micro-ondes; Imidazo[1,2-b]pyrazoles; Imidazo[1,2-a]imidazoles; Imidazo[1,2-a]imidazolin-2-ones; Direct (hetero)arylation; Metallo-catalysed reactions; Regioselectivity; Suzuki-Miyaura; Micro-waves

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Grosse, S. (2013). Imidazo[1, 2-b]pyrazoles, imidazo[1, 2-a]imidazoles : synthèse, fonctionnalisation et évaluation biologique : Imidazo[1,2-b]pyrazoles, imidazo[1,2-a]imidazoles : synthesis, functionalisation and biological evaluation. (Doctoral Dissertation). Université d'Orléans. Retrieved from http://www.theses.fr/2013ORLE2056

Chicago Manual of Style (16^th Edition):

Grosse, Sandrine. “Imidazo[1, 2-b]pyrazoles, imidazo[1, 2-a]imidazoles : synthèse, fonctionnalisation et évaluation biologique : Imidazo[1,2-b]pyrazoles, imidazo[1,2-a]imidazoles : synthesis, functionalisation and biological evaluation.” 2013. Doctoral Dissertation, Université d'Orléans. Accessed January 26, 2021. http://www.theses.fr/2013ORLE2056.

MLA Handbook (7^th Edition):

Grosse, Sandrine. “Imidazo[1, 2-b]pyrazoles, imidazo[1, 2-a]imidazoles : synthèse, fonctionnalisation et évaluation biologique : Imidazo[1,2-b]pyrazoles, imidazo[1,2-a]imidazoles : synthesis, functionalisation and biological evaluation.” 2013. Web. 26 Jan 2021.

Vancouver:

Grosse S. Imidazo[1, 2-b]pyrazoles, imidazo[1, 2-a]imidazoles : synthèse, fonctionnalisation et évaluation biologique : Imidazo[1,2-b]pyrazoles, imidazo[1,2-a]imidazoles : synthesis, functionalisation and biological evaluation. [Internet] [Doctoral dissertation]. Université d'Orléans; 2013. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2013ORLE2056.

Council of Science Editors:

Grosse S. Imidazo[1, 2-b]pyrazoles, imidazo[1, 2-a]imidazoles : synthèse, fonctionnalisation et évaluation biologique : Imidazo[1,2-b]pyrazoles, imidazo[1,2-a]imidazoles : synthesis, functionalisation and biological evaluation. [Doctoral Dissertation]. Université d'Orléans; 2013. Available from: http://www.theses.fr/2013ORLE2056

11. Marie, Emilie. Synthèse d'imidazo (1,2-a) pyridines à activité antivirale à l'encontre des virus de l'hépatite C et de la diarrhée virale bovine : Synthesis of imidazo[1,2-a]pyridines with antiviral activity against hepatisis C and bovine viral diarrhea viruses.

Degree: Docteur es, Sciences de la vie et de la santé, spécialité Chimie thérapeutique, 2012, Université François-Rabelais de Tours

URL: http://www.theses.fr/2012TOUR3802

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L’hépatite C est une maladie silencieuse, souvent asymptomatique, mais qui entraîne des lésions du foie et peut évoluer vers une cirrhose et, dans certains cas,… (more)

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L’hépatite C est une maladie silencieuse, souvent asymptomatique, mais qui entraîne des lésions du foie et peut évoluer vers une cirrhose et, dans certains cas, vers un cancer. Le carcinome hépatocellulaire engendré par l’hépatite C constitue la première cause de transplantation hépatique. Les virus de l’hépatite C (VHC) et de la diarrhée virale bovine (VDVB) sont deux pestivirus possédant un ARN monocaténaire, de la famille des Flaviviridae. Bien qu’ayant des génomes différents, ils présentent une organisation structurelle et des processus de développement de l’enveloppe cellulaire comparables. Le screening de la chimiothèque du laboratoire a permis d’identifier cinq composés chefs de files, actifs à l’encontre du virus de l’hépatite C. Deux de ces composés de la série imidazo[1,2-a]pyridine ont fait l’objet d’un travail de pharmacomodulation dans le cadre des thèses de Jean-Baptiste Véron et Nicolas Henry. La première partie de mon travail de recherche a donc consisté à poursuivre ces travaux de pharmacomodulation afin de tenter d’améliorer l’activité de cette série chimique à l’égard du VHC ainsi que son index thérapeutique. La synthèse convergente de ces molécules a été effectuée grâce à des couplages métallo-catalysés.La seconde partie de mon projet de recherche a porté sur l’étude de la bifonctionnalisation des positions 7 et 8 du noyau imidazo[1,2-a]pyridine. Ces travaux ont permis de développer de nouvelles méthodologies pour introduire une diversité fonctionnelle sur ces positions. Ces molécules ont également été évaluées à l’encontre du VHC et l’une d’entre elle a montré une activité intéressante à l’encontre de ce virus. L’activité à l’encontre du VHC et l’index thérapeutique ont été améliorés pour deux molécules, analogues du BPIP.

Hepatitis C is a silent disease, often asymptomatic, responsible for hepatic lesions which may lead to cirrhosis and in some cases, to cancer. Hepatocellular carcinoma caused by hepatitis C virus is the leading cause of liver transplantation. Bovine viral diarrhoea (BVDV) and hepatitis C (HCV) viruses are two pestiviruses from the Flaviviridae family that have a single-stranded RNA. Despite having different genomes, they present a similar structural organization and processes of development of the cell envelope.The laboratory’s chemical library screening has identified five hits, active against the HCV. Two of these compounds from the imidazo[1,2-a]pyridine serie were pharmacomodulated as part of the Ph.D. thesis of Jean-Baptiste Véron and Nicolas Henry.The first part of my research work was therefore to continue the pharmacomodulation study of these chemical series to improve their activity against HCV and their therapeutic index. To do so, the convergent synthesis of these molecules was performed using metal-catalyzed couplings.The second part of my project has focused on the study of the difunctionalization of positions 7 and 8 of the imidazo[1,2-a]pyridine nucleus. This work helped to develop new methodologies for introducing a functional diversity on these positions.…

Advisors/Committee Members: Gueiffier, Alain (thesis director).

Subjects/Keywords: Hépatite C; VHC; VDVB; Imidazo[1,2-a]pyridine; Pharmacomodulation; Bifonctionnalisation; Couplages métallo-catalysés; Évaluation biologique; Hepatitis C; HCV; BVDV; Imidazo [1,2-a]pyridine; Pharmacomodulation; Bifunctionalization; Metallo-catalyzed cross-coupling; Biological evaluation

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Marie, E. (2012). Synthèse d'imidazo (1,2-a) pyridines à activité antivirale à l'encontre des virus de l'hépatite C et de la diarrhée virale bovine : Synthesis of imidazo[1,2-a]pyridines with antiviral activity against hepatisis C and bovine viral diarrhea viruses. (Doctoral Dissertation). Université François-Rabelais de Tours. Retrieved from http://www.theses.fr/2012TOUR3802

Chicago Manual of Style (16^th Edition):

Marie, Emilie. “Synthèse d'imidazo (1,2-a) pyridines à activité antivirale à l'encontre des virus de l'hépatite C et de la diarrhée virale bovine : Synthesis of imidazo[1,2-a]pyridines with antiviral activity against hepatisis C and bovine viral diarrhea viruses.” 2012. Doctoral Dissertation, Université François-Rabelais de Tours. Accessed January 26, 2021. http://www.theses.fr/2012TOUR3802.

MLA Handbook (7^th Edition):

Marie, Emilie. “Synthèse d'imidazo (1,2-a) pyridines à activité antivirale à l'encontre des virus de l'hépatite C et de la diarrhée virale bovine : Synthesis of imidazo[1,2-a]pyridines with antiviral activity against hepatisis C and bovine viral diarrhea viruses.” 2012. Web. 26 Jan 2021.

Vancouver:

Marie E. Synthèse d'imidazo (1,2-a) pyridines à activité antivirale à l'encontre des virus de l'hépatite C et de la diarrhée virale bovine : Synthesis of imidazo[1,2-a]pyridines with antiviral activity against hepatisis C and bovine viral diarrhea viruses. [Internet] [Doctoral dissertation]. Université François-Rabelais de Tours; 2012. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2012TOUR3802.

Council of Science Editors:

Marie E. Synthèse d'imidazo (1,2-a) pyridines à activité antivirale à l'encontre des virus de l'hépatite C et de la diarrhée virale bovine : Synthesis of imidazo[1,2-a]pyridines with antiviral activity against hepatisis C and bovine viral diarrhea viruses. [Doctoral Dissertation]. Université François-Rabelais de Tours; 2012. Available from: http://www.theses.fr/2012TOUR3802

12. Oudot, Romain. Synthèse de dérivés imidazo[1,2-a] pyridines et imidazo[1,2-b] pyridazines tricycliques : Synthesis of imidazo[1,2-a] pyridines and imidazo[1,2-b] pyridazines tricyclic derivatives.

Degree: Docteur es, Sciences de la Vie et de la Santé, 2009, Université François-Rabelais de Tours

URL: http://www.theses.fr/2009TOUR3804

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Les motifs imidazo[1,2-a]pyridines et imidazo[1,2-b]pyridazines sont des noyaux très étudiés par la communauté scientifique, notamment dans le domaine thérapeutique. Ceci s’explique en partie par les… (more)

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Les motifs imidazo[1,2-a]pyridines et imidazo[1,2-b]pyridazines sont des noyaux très étudiés par la communauté scientifique, notamment dans le domaine thérapeutique. Ceci s’explique en partie par les progrès récents réalisés dans le domaine de la métallocatalyse qui ont permis une fonctionnalisation plus simple de ces molécules. Cependant, les dérivés tricycliques de ces structures sont restés assez peu étudiés malgré le fait que certains de leurs isostères présentent des propriétés biologiques intéressantes. Les travaux de cette thèse ont porté sur deux projets distincts : -La synthèse d’imidazo[1,2-b]pyridazines présentant un troisième cycle diazoté entre les positions 7 et 8, dans le cadre d’un contrat conclu avec la société Sanofi-Aventis. Ces composés, totalement originaux, représentent un véritable défi chimique et leur synthèse a nécessité d’importants travaux de mise au point. Nous avons ainsi employé différentes méthodes de couplages métallocatalysés. -La synthèse d’imidazo[1,2-a]pyridines un troisième cycle pyridinique entre les positions 2 et 3. Ces molécules, peu décrites dans la littérature, n’ont fait l’objet d’aucune évaluation biologique. Dans le but de synthétiser efficacement une chimiothèque intéressante pour ces structures, j’ai développé une méthode d’hétérocyclisation qui nous permet d’obtenir en deux étapes, gràce à des produits de départ très accessible, une importante variété de tricycles.

The imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines moeities are very studied by scientific community, specially in therapeutic field. This is mostly due to recent progress in metallocatalyzed couplings which allow easier functionnalization of these structures. However, the tricyclic derivatives of these compounds remained not very studied despite important biological properties of some of there isosters. This thesis is divided in two parts : -The synthesis of imidazo[1,2-b]pyridazines with a dinitrogenated third cycle between the positions 7 and 8 in collaboration with Sanofi-Aventis. These new compounds were a real chemical challenge and their synthesis required important works of development. We used various metallocatalyzed couplings methods. -The synthesis of imidazo[1,2-a]pyridines with a pyridinic cycle between the positions 2 and 3. These molecules, poorly described in the literature, have never been subject to biological study. In order to effectively synthesize an interesting range of these structures, I have developed a new heterocyclization method which allows us to obtain in two steps, starting from commercialy available starting materials, some original tricyclics compounds.

Advisors/Committee Members: Enguehard-Gueiffier, Cécile (thesis director).

Subjects/Keywords: Imidazo[1,2-a]pyridines; Imidazo[1,2-b]pyridazines; Tricycle; Métallocatalyse; Hétérocyclisation; Imidazo[1,2-a]pyridine; Imidazo[1,2-b]pyridazine; Tricyclic compounds; Metallocatalysis; Heterocyclization

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Oudot, R. (2009). Synthèse de dérivés imidazo[1,2-a] pyridines et imidazo[1,2-b] pyridazines tricycliques : Synthesis of imidazo[1,2-a] pyridines and imidazo[1,2-b] pyridazines tricyclic derivatives. (Doctoral Dissertation). Université François-Rabelais de Tours. Retrieved from http://www.theses.fr/2009TOUR3804

Chicago Manual of Style (16^th Edition):

Oudot, Romain. “Synthèse de dérivés imidazo[1,2-a] pyridines et imidazo[1,2-b] pyridazines tricycliques : Synthesis of imidazo[1,2-a] pyridines and imidazo[1,2-b] pyridazines tricyclic derivatives.” 2009. Doctoral Dissertation, Université François-Rabelais de Tours. Accessed January 26, 2021. http://www.theses.fr/2009TOUR3804.

MLA Handbook (7^th Edition):

Oudot, Romain. “Synthèse de dérivés imidazo[1,2-a] pyridines et imidazo[1,2-b] pyridazines tricycliques : Synthesis of imidazo[1,2-a] pyridines and imidazo[1,2-b] pyridazines tricyclic derivatives.” 2009. Web. 26 Jan 2021.

Vancouver:

Oudot R. Synthèse de dérivés imidazo[1,2-a] pyridines et imidazo[1,2-b] pyridazines tricycliques : Synthesis of imidazo[1,2-a] pyridines and imidazo[1,2-b] pyridazines tricyclic derivatives. [Internet] [Doctoral dissertation]. Université François-Rabelais de Tours; 2009. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2009TOUR3804.

Council of Science Editors:

Oudot R. Synthèse de dérivés imidazo[1,2-a] pyridines et imidazo[1,2-b] pyridazines tricycliques : Synthesis of imidazo[1,2-a] pyridines and imidazo[1,2-b] pyridazines tricyclic derivatives. [Doctoral Dissertation]. Université François-Rabelais de Tours; 2009. Available from: http://www.theses.fr/2009TOUR3804

13. Bou Karroum, Nour. Synthèse et développement de nouvelles molécules hétérocycliques tricycliques : étude de leurs propriétés immunomodulatrices : Synthesis and development of novel tricyclic heterocyclic molecules : study of their immunomodulatory properties.

Degree: Docteur es, Biologie Santé, 2018, Montpellier; École Doctorale des Sciences et de Technologie (Beyrouth)

URL: http://www.theses.fr/2018MONTT014

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Les récepteurs Toll-like 7 et 8 jouent un rôle important dans l’activation de la réponse immunitaire innée et adaptative. Leur stimulation conduit à la production… (more)

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Les récepteurs Toll-like 7 et 8 jouent un rôle important dans l’activation de la réponse immunitaire innée et adaptative. Leur stimulation conduit à la production des cytokines pro-inflammatoires et d’interférons de type I. L’imiquimod et son dérivé le résiquimod sont les premières molécules de faible poids moléculaire décrites comme agonistes du TLR7 et TLR8. Ces deux molécules ont montré des activités anticancéreuses et adjuvantes très importantes. Récemment, les TLR 7 et 8 ont fait l’objet de plusieurs publications visant à développer de nouveaux agonistes TLR7 et/ou TLR8 dans la perspective d’être utilisés comme adjuvants vaccinaux. Malgré les rôles essentiels de TLR7 et TLR8 dans la stimulation du système immunitaire, une activation immunitaire chronique peut être responsable de plusieurs maladies infectieuses et auto-immunes. D’où l’importance de développer également des antagonistes TLR7 et/ou TLR8.Ce travail de thèse est consacré à la synthèse et le développement de nouvelles molécules hétérocycliques, analogues de l’imiquimod et de résiquimod, dans le but d’identifier de nouveaux ligands TLR7 et/ou TLR8. Des voies de synthèse innovantes, permettant une modulation chimique importante grâce à des couplages croisés pallado-catalysés, ont été mises au point et ont permis d’obtenir une cinquantaine de molécules appartenant à trois séries chimiques différentes de type imidazo[1,2-a]pyrazine, imidazo[1,5-a]quinoxaline et pyrazolo[1,5-a]quinoxaline. De nombreux essais d’alkylation ont été tentés sur ces trois séries chimiques afin d’introduire une large variété de substituants sur le cycle à cinq sommets. L’application du couplage croisé de Sonogashira nous a permis d’établir une liaison C-C et introduire diverses chaines alkyles. Ces composés ont été testés pour leur activité agoniste et antagoniste TLR7 et 8. Aucun des composés cibles n'a présenté d’activité agoniste TLR7 et TLR8, dans l'intervalle des concentrations testées. Par contre, tous les composés ont montré une activité antagoniste sélective du TLR7. Les composés les plus actifs, 5.35a et 5.35b, membres de la série pyrazolo[1,5-a]quinoxaline ont montré des IC50 de l’ordre de 10 μM. Ces résultats prometteurs nous ont permis la découverte d’une activité antagoniste TLR7 importante pour la série pyrazolo[1,5-a]quinoxaline, une série très peu développée dans la littérature. La modulation chimique des molécules actives nous permet de donner naissance à de nouveaux leaders, qui peuvent jouer un rôle important dans la thérapie de plusieurs maladies infectieuses et auto-immunes.

Toll-like receptors 7 and 8 play an important role in immune system activation. Their stimulation leads to the production of pro-inflammatory cytokines and type I interferons. Both receptors recognize viral ssRNA, as well as synthetic tricyclic imidazoquinoline derivatives such as imiquimod (TLR7 agonist) and resiquimod (TLR7/8 agonist). These two molecules showed significative anti-cancer and adjuvant activities. Many reports in the literature have been focused on the development of…

Advisors/Committee Members: Bonnet, Pierre-Antoine (thesis director), Kassab, Issam (thesis director).

Subjects/Keywords: Imidazo[1; 5-A]quinoxaline; Pyrazolo[1; 5-A]quinoxaline; Immunomodulation; Toll-Like receptor 7 et 8 (TLR7/8); Ligands TLR7 et TLR8; Imidazo[1; 2-A]pyrazine; Imidazo[1;

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Bou Karroum, N. (2018). Synthèse et développement de nouvelles molécules hétérocycliques tricycliques : étude de leurs propriétés immunomodulatrices : Synthesis and development of novel tricyclic heterocyclic molecules : study of their immunomodulatory properties. (Doctoral Dissertation). Montpellier; École Doctorale des Sciences et de Technologie (Beyrouth). Retrieved from http://www.theses.fr/2018MONTT014

Chicago Manual of Style (16^th Edition):

Bou Karroum, Nour. “Synthèse et développement de nouvelles molécules hétérocycliques tricycliques : étude de leurs propriétés immunomodulatrices : Synthesis and development of novel tricyclic heterocyclic molecules : study of their immunomodulatory properties.” 2018. Doctoral Dissertation, Montpellier; École Doctorale des Sciences et de Technologie (Beyrouth). Accessed January 26, 2021. http://www.theses.fr/2018MONTT014.

MLA Handbook (7^th Edition):

Bou Karroum, Nour. “Synthèse et développement de nouvelles molécules hétérocycliques tricycliques : étude de leurs propriétés immunomodulatrices : Synthesis and development of novel tricyclic heterocyclic molecules : study of their immunomodulatory properties.” 2018. Web. 26 Jan 2021.

Vancouver:

Bou Karroum N. Synthèse et développement de nouvelles molécules hétérocycliques tricycliques : étude de leurs propriétés immunomodulatrices : Synthesis and development of novel tricyclic heterocyclic molecules : study of their immunomodulatory properties. [Internet] [Doctoral dissertation]. Montpellier; École Doctorale des Sciences et de Technologie (Beyrouth); 2018. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2018MONTT014.

Council of Science Editors:

Bou Karroum N. Synthèse et développement de nouvelles molécules hétérocycliques tricycliques : étude de leurs propriétés immunomodulatrices : Synthesis and development of novel tricyclic heterocyclic molecules : study of their immunomodulatory properties. [Doctoral Dissertation]. Montpellier; École Doctorale des Sciences et de Technologie (Beyrouth); 2018. Available from: http://www.theses.fr/2018MONTT014

14. Bahlaouan, Zineb. Réactivité cupro-catalysée des systèmes mono, di et triiodés porteurs d'une fonction acide carboxylique ou dérivée : applications à la synthèse de nouveaux hétérocycles. : Copper-catalysed reactive systems mono, di and tri-iodo compound carrying a carboxylic acid or derivatives : applications to the synthesis of new heterocycles.

Degree: Docteur es, Chimie organique, 2011, Université François-Rabelais de Tours

URL: http://www.theses.fr/2011TOUR4035

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Les hétérocycles oxygénés, azotés et soufrés sont des motifs présents dans de nombreux produits naturels possédant des activités biologiques intéressantes. Plusieurs publications décrivant la synthèse… (more)

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Les hétérocycles oxygénés, azotés et soufrés sont des motifs présents dans de nombreux produits naturels possédant des activités biologiques intéressantes. Plusieurs publications décrivant la synthèse de ces hétérocycles en particulier oxygénés et azotés reposent sur l’utilisation des métaux de transition en tant que catalyseur.Dans notre cas, nous nous sommes intéressés dans un premier temps à la synthèse cupro-catalysée des pyrano[3’,4’:4,5]imidazo[1,2-a]pyridin-1-ones selon une réaction tandem impliquant un couplage et une hétérocyclisation, à partir des dérivés de l’acide 3-iodo-, 3,6- ou (3,8) diiodoimidazo[1,2-a]pyridine-2-carboxylique et d’alcynes vrais en présence de sels de cuivre (I) dans le DMF. Les réactions développées ne nécessitent aucune utilisation de métaux de transition plus coûteux comme les complexes au palladium par exemple.

Heterocycles of oxygen, nitrogen and sulfur are patterns found in many natural products possessing interesting biological activities. Several researchers describe the synthesis of oxygen and nitrogen based heterocycles using transition metals as catalyst.In the present study, we focused initially on the copper-catalyzed synthesis of pyrano[3',4':4,5]imidazo[1,2-a]pyridin-1-ones by a tandem coupling-heterocyclisation reaction from derivatives of 3-iodo-, 3,6- or (3,8) diiodoimidazo[1,2-a]pyridine-2-carboxylic acid and terminal alkynes in the presence of copper (I) salts as catalyst in DMF. This procedure does not require the use of any expensive transition metal complexes like palladium and supplement any additives. The extension of this methodology to 2,3,5-triiodobenzoic acid allowed the regioselective synthesis of new isocoumarins substituted in positions 3, 5 and 7. Regioselective reactivity of iodine atoms in position 5 and 7 has been studied by palladium coupling reactions and nucleophilic substitution to broad its synthesis to a wide variety of new substituted isocoumarins.

Advisors/Committee Members: Abarbri, Mohamed (thesis director).

Subjects/Keywords: Allènyltributylétains; Couplage; Imidazo[1,2-a]pyridinones; Isocoumarines; Stéréosélectivité; Pyrano[3,4-b]indole-1(9H)-one; 1,1-dioxyde-benzothiazin-3-ones; Copper (I); Catalyst; Imidazo[1,2-a]pyridinones; Regioselectivity; Stereoselectivity; Isocoumarins; Allenyltributyltin; Sulfonamides; N-Arylation; Pyrano[3,4-b]indole-1(9H)-one; Benzothiazin-3-one-1,1-dioxyde

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Bahlaouan, Z. (2011). Réactivité cupro-catalysée des systèmes mono, di et triiodés porteurs d'une fonction acide carboxylique ou dérivée : applications à la synthèse de nouveaux hétérocycles. : Copper-catalysed reactive systems mono, di and tri-iodo compound carrying a carboxylic acid or derivatives : applications to the synthesis of new heterocycles. (Doctoral Dissertation). Université François-Rabelais de Tours. Retrieved from http://www.theses.fr/2011TOUR4035

Chicago Manual of Style (16^th Edition):

Bahlaouan, Zineb. “Réactivité cupro-catalysée des systèmes mono, di et triiodés porteurs d'une fonction acide carboxylique ou dérivée : applications à la synthèse de nouveaux hétérocycles. : Copper-catalysed reactive systems mono, di and tri-iodo compound carrying a carboxylic acid or derivatives : applications to the synthesis of new heterocycles.” 2011. Doctoral Dissertation, Université François-Rabelais de Tours. Accessed January 26, 2021. http://www.theses.fr/2011TOUR4035.

MLA Handbook (7^th Edition):

Bahlaouan, Zineb. “Réactivité cupro-catalysée des systèmes mono, di et triiodés porteurs d'une fonction acide carboxylique ou dérivée : applications à la synthèse de nouveaux hétérocycles. : Copper-catalysed reactive systems mono, di and tri-iodo compound carrying a carboxylic acid or derivatives : applications to the synthesis of new heterocycles.” 2011. Web. 26 Jan 2021.

Vancouver:

Bahlaouan Z. Réactivité cupro-catalysée des systèmes mono, di et triiodés porteurs d'une fonction acide carboxylique ou dérivée : applications à la synthèse de nouveaux hétérocycles. : Copper-catalysed reactive systems mono, di and tri-iodo compound carrying a carboxylic acid or derivatives : applications to the synthesis of new heterocycles. [Internet] [Doctoral dissertation]. Université François-Rabelais de Tours; 2011. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2011TOUR4035.

Council of Science Editors:

Bahlaouan Z. Réactivité cupro-catalysée des systèmes mono, di et triiodés porteurs d'une fonction acide carboxylique ou dérivée : applications à la synthèse de nouveaux hétérocycles. : Copper-catalysed reactive systems mono, di and tri-iodo compound carrying a carboxylic acid or derivatives : applications to the synthesis of new heterocycles. [Doctoral Dissertation]. Université François-Rabelais de Tours; 2011. Available from: http://www.theses.fr/2011TOUR4035

15. Mayne, Christopher G. Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function.

Degree: PhD, 0335, 2011, University of Illinois – Urbana-Champaign

URL: http://hdl.handle.net/2142/24514

► A member of the nuclear receptor superfamily, the estrogen receptor (ER) is a ligand-regulated transcription factor responsible for the regulation of hundreds of genes. Consequently,… (more)

▼ A member of the nuclear receptor superfamily, the estrogen receptor (ER) is a ligand-regulated transcription factor responsible for the regulation of hundreds of genes. Consequently, ERs are involved in numerous disease states, including cellular proliferation, post-menopausal symptoms, inflammation, and neurodegeneration, all of which represent potential opportunities for endocrine therapies. Sustained efforts in structural biology have led to the deposition of many high resolution x-ray crystal structures of ligand-receptor complexes into the PDB, and provide valuable insight into the key ligand-receptor interactions determining binding affinity and, in some cases, specific macroscopic structural attributes that directly affect ER function. As described herein, we have leveraged selected PDB structures, supplemented by additional unpublished structures obtained from collaborators, to design and develop chemical probes of ER function. The underlying mechanisms driving ligand affinity and selectivity remain a key focus in understanding ER function. Correspondingly, we describe the development of imidazo[1,2-a]pyridine ligands to probe the importance of the core scaffold structure in ligand binding affinity. Computational analysis of ligand and receptor structures has led to the identification of the interaction between their respective dipole moments as an important receptor-ligand interaction. We also set out to discover novel ER scaffolds through a virtual screening approach and follow-up synthetic efforts to identify and further investigate a thiadiazole scaffold bearing an extended alkyl substituent. Docking structures suggest an intriguing binding mode probing the presence of a putative second binding volume reminiscent of that observed for the high affinity and highly selective glucocorticoid receptor (GR) ligand, deacylcortivazol (DAC). The diverse biological roles of ERs also provide opportunities to probe receptor function through alternative mechanisms. We report the use of recent crystal structures to design novel modifications of known ER ligands in probing the molecular basis for receptor crosstalk between ER and NF-??B, and the resulting effect on inflammatory pathways. These ligand modifications are centered on destabilizing helix 12 by disrupting the position of a single histidine residue within the binding pocket, and have been shown to effect antagonist activity on both classical ER pathways and the expression of IL-6, the latter being representative of inflammatory responses, in vivo. Previous work in our labs has also demonstrated that the assessment of ER-dependent targets can provide a better indication of ER function in vivo than assaying ER itself. To this end, we have developed new scoring functions for evaluating docked structures of fluorinated analogues of Tanaproget for the progesterone receptor (PR), whose expression is tightly controlled by ER. These functions have been applied in the design and selection of new synthetic targets for use in imaging ER-positive tumors via… Advisors/Committee Members: Katzenellenbogen, John A. (advisor), Katzenellenbogen, John A. (Committee Chair), Hergenrother, Paul J. (committee member), Nardulli, Ann M. (committee member), Burke, Martin D. (committee member).

Subjects/Keywords: Estrogen Receptor; Imidazo[1,2-a]pyridine; oxabicycloheptene; estradiol; thiadiazole; steroid; Progesterone Receptor; Tanaproget

…Synthesis of Imidazo[1,2-a]pyridine Scaffold O NH2 + N N EtOH Br N reflux 1, 71… …2005, 48, 5092. 14 CHAPTER 2 THE DESIGN AND SYNTHESIS OF IMIDAZO[1,2-a]PYRIDINES… …Chloroindazole OH OH N Imidazo[1,2-a]pyridine Scaffold Core HO ER!-selective… …replaced by an imidazo[1,2-a]pyridine. Both of these structures adhere to the general… …intermediates. Figure 2.2. Retrosynthetic Analysis of Imidazo[1,2-a]pyridine Core and…

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Mayne, C. G. (2011). Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function. (Doctoral Dissertation). University of Illinois – Urbana-Champaign. Retrieved from http://hdl.handle.net/2142/24514

Chicago Manual of Style (16^th Edition):

Mayne, Christopher G. “Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function.” 2011. Doctoral Dissertation, University of Illinois – Urbana-Champaign. Accessed January 26, 2021. http://hdl.handle.net/2142/24514.

MLA Handbook (7^th Edition):

Mayne, Christopher G. “Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function.” 2011. Web. 26 Jan 2021.

Vancouver:

Mayne CG. Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function. [Internet] [Doctoral dissertation]. University of Illinois – Urbana-Champaign; 2011. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/2142/24514.

Council of Science Editors:

Mayne CG. Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function. [Doctoral Dissertation]. University of Illinois – Urbana-Champaign; 2011. Available from: http://hdl.handle.net/2142/24514

16. Al-bashabsheh, Zaher Qassim. The inhibitory effect of natural antioxidants on formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in a model system.

Degree: PhD, Food Science Institute, 2019, Kansas State University

URL: http://hdl.handle.net/2097/39596

► Heterocyclic amines (HCAs) are a class of mutagenic and carcinogenic compounds generated when muscle foods are cooked at high temperatures. Exposure to HCAs has been… (more)

▼ Heterocyclic amines (HCAs) are a class of mutagenic and carcinogenic compounds generated when muscle foods are cooked at high temperatures. Exposure to HCAs has been linked to human cancers, among them colon, prostate, breast, and pancreatic cancers. Research has focused recently on how HCAs form and how their formation can be inhibited. 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP) is a common, potentially harmful HCA that forms via the Maillard reaction. The health consequences of consuming HCAs has caused the International Agency for Research on Cancer (IARC) to list PhIP as a “possible human carcinogen.” Antioxidant spices and flavonoid compounds have received considerable attention for their beneficial effect against HCA formation in our daily foods. Consumption of most these antioxidants has been found to protect against various chronic diseases such as cardiovascular diseases and cancers. Chemical model systems help in assessing how HCA formation can be inhibited using different compounds. Chemical model systems are preferred because they limit side reactions that occur in meats, complicating analysis, and thus allow studying the chemical interactions among the precursors of HCAs and applied antioxidants. In this research a model system with 0.011 mmol glucose, 0.022 mmol creatinine, and 0.022 mmol phenylalanine in 90:10 diethylene glycol/water (v/v) was heat-treated at 180°C for 1 hour to test the formation of PhIP. Black and red pepper compounds such as pepper oil, piperine, D-limonene, P-cymene, and capsaicin and flavonoid compounds such as quercetin, apigenin, genistin, phlorizin, and catechin were added individually to the model system at three concentrations (125, 625, and 1250 ppm) to test their effect on PhIP formation. The PhIP contents were assessed using HPLC. The results indicate that four out of five antioxidant components of spices: black pepper oil, piperine, D-limonene, and capsaicin significantly (p < 0.05) reduced PhIP formation, while P-cymene had no significant effect on PhIP formation. All flavonoid compounds also had a significant (p < 0.05) effect on PhIP formation. In addition, binary combinations of two antioxidant spices such as piperine and capsaicin and two flavonoid compounds such as genistin and catechin at 1:0.25, 1:0.5, and 1:1 ratios were also evaluated. Significant (p < 0.05) synergistic effects were observed among all combinations. Our results showed that when antioxidant spices and flavonoid compounds were added to model systems either individually or in combination, they reduced PhIP formation. These findings provide valuable information about antioxidant spices and flavonoid compounds as protective agents against HCA formation. Advisors/Committee Members: J. Scott Smith.

Subjects/Keywords: Heterocyclic amine; 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine; Spices; Flavonoid compounds; Model system

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APA (6^th Edition):

Al-bashabsheh, Z. Q. (2019). The inhibitory effect of natural antioxidants on formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in a model system. (Doctoral Dissertation). Kansas State University. Retrieved from http://hdl.handle.net/2097/39596

Chicago Manual of Style (16^th Edition):

Al-bashabsheh, Zaher Qassim. “The inhibitory effect of natural antioxidants on formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in a model system.” 2019. Doctoral Dissertation, Kansas State University. Accessed January 26, 2021. http://hdl.handle.net/2097/39596.

MLA Handbook (7^th Edition):

Al-bashabsheh, Zaher Qassim. “The inhibitory effect of natural antioxidants on formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in a model system.” 2019. Web. 26 Jan 2021.

Vancouver:

Al-bashabsheh ZQ. The inhibitory effect of natural antioxidants on formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in a model system. [Internet] [Doctoral dissertation]. Kansas State University; 2019. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/2097/39596.

Council of Science Editors:

Al-bashabsheh ZQ. The inhibitory effect of natural antioxidants on formation of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) in a model system. [Doctoral Dissertation]. Kansas State University; 2019. Available from: http://hdl.handle.net/2097/39596

17. Kelly, Elizabeth A. Formation and inhibition of the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in a model system.

Degree: MS, Food Science - Animal Sciences and Industry, 2015, Kansas State University

URL: http://hdl.handle.net/2097/20520

► Heterocyclic amines (HCAs) are a class of mutagenic and carcinogenic chemical compounds formed on the outside of meat and fish when cooked at high temperatures.… (more)

Subjects/Keywords: 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine; Heterocyclic amine; Model system; Black pepper; Inhibition; Food Science (0359)

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Kelly, E. A. (2015). Formation and inhibition of the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in a model system. (Masters Thesis). Kansas State University. Retrieved from http://hdl.handle.net/2097/20520

Chicago Manual of Style (16^th Edition):

Kelly, Elizabeth A. “Formation and inhibition of the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in a model system.” 2015. Masters Thesis, Kansas State University. Accessed January 26, 2021. http://hdl.handle.net/2097/20520.

MLA Handbook (7^th Edition):

Kelly, Elizabeth A. “Formation and inhibition of the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in a model system.” 2015. Web. 26 Jan 2021.

Vancouver:

Kelly EA. Formation and inhibition of the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in a model system. [Internet] [Masters thesis]. Kansas State University; 2015. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/2097/20520.

Council of Science Editors:

Kelly EA. Formation and inhibition of the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in a model system. [Masters Thesis]. Kansas State University; 2015. Available from: http://hdl.handle.net/2097/20520

18. Lavrard-Meyer, Hubert. Synthèse et fonctionnalisation du motif pyridine-[b]-bicyclique : Synthesis and functionalization of [b]-fused pyridine compounds.

Degree: Docteur es, Chimie organique, 2017, Lyon

URL: http://www.theses.fr/2017LYSE1186

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Une multitude de composés organiques présente une structure bicyclique azotée insaturée.Parmi ceux-ci, le motif pyridine-[b]-bicyclique est extrêmement fréquent, et se compose d’unepyridine accolée à un… (more)

Subjects/Keywords: Hétérocycle; Quinoline; Pyrazolo[3,4-b]pyridine; Imidazo[4,5-b]pyridine; Palladium; Couplage croisé; C-H activation; Heterocycle; Quinoline; Pyrazolo[3,4-b]pyridine; Imidazo[4,5-b]pyridine; Palladium; Cross-coupling; C-H activation; 547

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Lavrard-Meyer, H. (2017). Synthèse et fonctionnalisation du motif pyridine-[b]-bicyclique : Synthesis and functionalization of [b]-fused pyridine compounds. (Doctoral Dissertation). Lyon. Retrieved from http://www.theses.fr/2017LYSE1186

Chicago Manual of Style (16^th Edition):

Lavrard-Meyer, Hubert. “Synthèse et fonctionnalisation du motif pyridine-[b]-bicyclique : Synthesis and functionalization of [b]-fused pyridine compounds.” 2017. Doctoral Dissertation, Lyon. Accessed January 26, 2021. http://www.theses.fr/2017LYSE1186.

MLA Handbook (7^th Edition):

Lavrard-Meyer, Hubert. “Synthèse et fonctionnalisation du motif pyridine-[b]-bicyclique : Synthesis and functionalization of [b]-fused pyridine compounds.” 2017. Web. 26 Jan 2021.

Vancouver:

Lavrard-Meyer H. Synthèse et fonctionnalisation du motif pyridine-[b]-bicyclique : Synthesis and functionalization of [b]-fused pyridine compounds. [Internet] [Doctoral dissertation]. Lyon; 2017. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2017LYSE1186.

Council of Science Editors:

Lavrard-Meyer H. Synthèse et fonctionnalisation du motif pyridine-[b]-bicyclique : Synthesis and functionalization of [b]-fused pyridine compounds. [Doctoral Dissertation]. Lyon; 2017. Available from: http://www.theses.fr/2017LYSE1186

19. Μαζαρακιώτη, Ελένη. Σύμπλοκες ενώσεις του καδμίου(ΙΙ) και των λανθανιδίων(ΙΙΙ) με οξιμικούς, υδραζονικούς και ετεροκυκλικούς υποκαταστάτες.

Degree: 2013, University of Patras

URL: http://hdl.handle.net/10889/6199

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Ο αρχικός στόχος της εργασίας μας ήταν η παρασκευή ετερομεταλλικών συμπλόκων Cd(II)/Ln(III) [Ln=λανθανίδιο] για να μελετηθούν οι φωτοφυσικές τους ιδιότητες. Διάφορα συστήματα αντιδράσεων Cd(II)/Ln(III)/οργανικός υποκαταστάτης… (more)

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Ο αρχικός στόχος της εργασίας μας ήταν η παρασκευή ετερομεταλλικών συμπλόκων Cd(II)/Ln(III) [Ln=λανθανίδιο] για να μελετηθούν οι φωτοφυσικές τους ιδιότητες. Διάφορα συστήματα αντιδράσεων Cd(II)/Ln(III)/οργανικός υποκαταστάτης έδωσαν μόνο ομομεταλλικές ενώσεις Cd(II) ή Pr(III).Χρησιμοποιώντας διάφορα αντιδρώντα Cd(II) και Pr(NO3)3∙6H2O, παρασκευάστηκαν τα ακόλουθα σύμπλοκα: [CdCl2(PhpaoH)]n (1), [Cd(O2CMe)2(NH2paoH)2] (2), [Cd(ΝΟ3)2(tzpy)2] (3), [CdI2(tzpy)2] (4), [Pr(ΝΟ3)3(tzpy)2]∙tzpy (5∙tzpy), [Cd4(NO3)4{(py)2C(H)(O)}4] (6) [(py)2C(H)(O)- είναι το ανιόν της δι-2-πυρίδυλο μεθανόλης που σχηματίζεται in-situ από τη μεταλλο-υποβοηθούμενη αναγωγή της (py)2CO με MeOH κάτω από σολβοθερμικές συνθήκες], [Cd(ΝΟ3)2(aphz)2] (7), [CdI2(aphz)2]n (8), [Pr(ΝΟ3)3(aphz)2] (9), [CdI2(bphz)2] (10), [Cd(NO3)2(bzdhz)2] (11). Η αντίδραση του Pr(NO3)3∙6H2O με δύο ισοδύναμα bzdhz σε H2O/Me2CO οδήγησε στην απομόνωση της Ν,Ν’-δι-ισοπροπυλιδενε-βενζίλιο διυδραζόνη (L’). Οι δομές των ενώσεων 1-11 προσδιορίσθηκαν με κρυσταλλογραφία ακτίνων Χ μονοκρυστάλλου. Όλα τα σύμπλοκα χαρακτηρίσθηκαν με φασματοσκοπία IR, και επιλεγμένες ενώσεις με τεχνικές RAMAN και 1H NMR. Τα φασματοσκοπικά δεδομένα εξετάζονται σε σχέση με τις γνωστές δομές των ενώσεων και των τρόπων ένταξης των υποκαταστατών.Πιστεύουμε ότι τα αποτελέσματα που παρουσιάζονται στη Διπλωματική Εργασία συνιστούν συνεισφορά στη χημεία του καδμίου(ΙΙ) και του πρασεοδυμίου(ΙΙΙ), καθώς επίσης και στη χημεία ένταξης των οργανικών υποκαταστατών.

The original goal of this work was to prepare heterometallic Cd(II)/Ln(III) complexes (Ln=lanthanide) in order to study their photophysical properties. A variety of CdII/PrIII/organic ligand reaction schemes led to only homometallic Cd(II) or Pr(III) complexes.Employing various Cd(II) sources and Pr(NO3)3∙6H2O, as starting materials, the following complexes have been prepared: [CdCl2(PhpaoH)]n (1), [Cd(O2CMe)2(NH2paoH)2] (2), [Cd(ΝΟ3)2(tzpy)2] (3), [CdI2(tzpy)2] (4), [Pr(ΝΟ3)3(tzpy)2]∙tzpy (5∙tzpy), [Cd4(NO3)4{(py)2C(H)(O)}4] (6) [(py)2C(H)(O)- is the anion of di-2-pyridyl methanol formed in-situ by the metal ion-assisted reduction of (py)2CO in MeOH under solvothermal conditions], [Cd(ΝΟ3)2(aphz)2] (7), [CdI2(aphz)2]n (8), [Pr(ΝΟ3)3(aphz)2] (9), [CdI2(bphz)2] (10), [Cd(NO3)2(bzdhz)2] (11). The reaction of Pr(NO3)3∙6H2O and 2 equivalents of bzdhz in H2O/Me2CO led to the isolation of N,N’-di-isopropylidene-benzil dihydrazone (L’). The structures of 1-11 and L’ have been determined by single-crystal X-ray crystallography. All the complexes have been characterized by IR spectroscopy, and selected compounds by RAMAN and 1H NMR techniques. The spectroscopic data are discussed in terms of the known structures and the coordination modes of the ligands.We believe that our results contribute into the chemistry of cadmium(II) and the praseodymium(III), and into the coordination chemistry.

Advisors/Committee Members: Περλεπές, Σπυρίδων, Mazarakioti, Eleni, Περλεπές, Σπυρίδων, Ψυχάρης, Βασίλειος, Μπόκιας, Γεώργιος.

Subjects/Keywords: Βενζίλιο διυδραζόνη; Ν,Ν’-δι-ισοπροπυλιδενε-βενζίλιο διυδραζόνη; Δι-2-πυρίδυλο μεθανόλη ως υποκαταστάτης; Κάδμιο(ΙΙ); Κρυσταλλογραφία ακτίνων Χ μονοκρυστάλλου; Πρασεοδύμιο(ΙΙΙ); 2-πυρίδυλο οξίμες; 3-(2-πυριδυλο)τριαζολο[1,5-a]πυριδίνη; 2-πυρίδυλο υδραζόνες; Σολβοθερμικές αντιδράσεις; Φασματοσκοπικές τεχνικές; Χημεία ένταξης; 546; Benzil dihydrazone; N, N'-di-isopropylidene-benzil dihydrazone; Di-2-pyridyl methanol as ligand; Cadmium(II); Single-crystal X-ray crystallography; Praseodymium(III); 2-pyridyl hydrazone; 3-(2-pyridyl)triazolo[1, 5-a]pyridine; 2-pyridyl oximes; Solvothermal reactions; Infrared spectroscopy (IR spectroscopy); Raman spectroscopy; Proton NMR (1H NMR); Coordination chemistry

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Μαζαρακιώτη, �. (2013). Σύμπλοκες ενώσεις του καδμίου(ΙΙ) και των λανθανιδίων(ΙΙΙ) με οξιμικούς, υδραζονικούς και ετεροκυκλικούς υποκαταστάτες. (Masters Thesis). University of Patras. Retrieved from http://hdl.handle.net/10889/6199

Chicago Manual of Style (16^th Edition):

Μαζαρακιώτη, Ελένη. “Σύμπλοκες ενώσεις του καδμίου(ΙΙ) και των λανθανιδίων(ΙΙΙ) με οξιμικούς, υδραζονικούς και ετεροκυκλικούς υποκαταστάτες.” 2013. Masters Thesis, University of Patras. Accessed January 26, 2021. http://hdl.handle.net/10889/6199.

MLA Handbook (7^th Edition):

Μαζαρακιώτη, Ελένη. “Σύμπλοκες ενώσεις του καδμίου(ΙΙ) και των λανθανιδίων(ΙΙΙ) με οξιμικούς, υδραζονικούς και ετεροκυκλικούς υποκαταστάτες.” 2013. Web. 26 Jan 2021.

Vancouver:

Μαζαρακιώτη �. Σύμπλοκες ενώσεις του καδμίου(ΙΙ) και των λανθανιδίων(ΙΙΙ) με οξιμικούς, υδραζονικούς και ετεροκυκλικούς υποκαταστάτες. [Internet] [Masters thesis]. University of Patras; 2013. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/10889/6199.

Council of Science Editors:

Μαζαρακιώτη �. Σύμπλοκες ενώσεις του καδμίου(ΙΙ) και των λανθανιδίων(ΙΙΙ) με οξιμικούς, υδραζονικούς και ετεροκυκλικούς υποκαταστάτες. [Masters Thesis]. University of Patras; 2013. Available from: http://hdl.handle.net/10889/6199

20. Bendjeddou, Lyamin. Synthèse et évaluation biologique de nouveaux inhibiteurs de kinases : identification d‘inhibiteurs de kinases parasitaires : Synthesis and biological evaluation of new kinase inhibitors : identification of inhibitors of several parasite protein kinases.

Degree: Docteur es, Chimie thérapeutique, 2014, Université Paris Descartes – Paris V

URL: http://www.theses.fr/2014PA05P615

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La phosphorylation des protéines par les kinases est l’une plus importantes modification post-traductionnelle dans les processus cellulaires tels que la division, la différenciation, la prolifération… (more)

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La phosphorylation des protéines par les kinases est l’une plus importantes modification post-traductionnelle dans les processus cellulaires tels que la division, la différenciation, la prolifération et l’apoptose. Due à leur rôle clef, un dérèglement des protéines kinases peut entrainer de nombreuses pathologies proliférative telles que le cancer et non prolifératives telles que les maladies neurodégénératives. Le travail de thèse s’est construit autour de 2 séries d’inhibiteurs de protéine kinases comportant les noyaux imidazo[1,2-b]pyridazine et imidazo[4,5-b]pyridine. L’objectif est d’inhiber sélectivement les protéines kinases choisies, pour leurs implications dans les pathologies visées au laboratoire. Les imidazo[1,2-b]pyridazines ont été préparées pour identifier des inhibiteurs de CLK1 et DYRK1A, cibles potentielles dans la maladie d’Alzheimer. Parmi les imidazo[1,2-b]pyridazines synthétisées, plusieurs molécules se sont révélées particulièrement sélectives de DYRKs et CLKs, avec des IC50 < 100 nM. Une relation structure-activité basée sur la synthèse de 70 molécules, a permis de dégager des éléments structuraux de la sélectivité des molécules. L’évaluation des produits a également été portée sur les kinases de parasites. Il a ainsi été possible d’identifier quelques inhibiteurs actifs sur PfCLK1. La seconde partie de cette thèse avait pour objectif l’optimisation du protocole de synthèse imidazo[4,5-b]pyridines, analogue de la roscovitine. Des dérivés s’étaient révélés capables d’inhiber la formation de kystes, dans un modèle cellulaire de polykystose rénale. Une synthèse en sept étapes a conduit à plusieurs grammes d’imidazo[4,5-b]pyridine 3,5,7 trisubstitués, qui sont ainsi disponibles pour l’évaluation in vivo.

Phosphorylation by protein kinases is one of the most important post-translational modification in cellular processes such as division, differentiation, proliferation and apoptosis. Kinase deregulation is associated with numerous diseases such as cancer or neurodegenerative diseases. Imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine were prepared to inhibit protein kinases involved in diseases targeted in the laboratory. The imidazo[1,2-b]pyridazines were synthesized to identify inhibitors of CLK1 and DYRK1A, potential targets in Alzheimer's disease. Among the imidazo[1,2-b]pyridazines synthesized, several molecules were found selective of DYRKs and CLKs, with IC50 < 100 nM. A structure-activity relationship based on the synthesis of 70 molecules, led to the identification of the structural bases of the selectivity. Products were also evaluated against parasite kinases. It was possible to identify some highly potent inhibitors on PfCLK1. The aim of second part of this thesis was to optimize the synthetic process to obtain imidazo[4,5-b]pyridines, which are close analogues of roscovitine. Derivatives had proved capable of inhibiting the formation of cysts in a cellular model of polycystic kidney disease. A seven-step synthesis has led to several grams of 3,5,7-trisubstituted…

Advisors/Committee Members: Galons, Hervé (thesis director).

Subjects/Keywords: Inhibiteur de protéine kinase; Imidazo[1,2-b]pyridazine; Imidazo[4,5-b]pyridine; Kinase cycline-dépendante (CDKs); CDC-like kinase (CLKs); Dual specificity tyrosine-phosphorylation-regulated kinase (DYRKs); Parasite unicellulaire; Maladie d’Alzheimer; Trisomie 21; Kinase inhibitor; Imidazo[1,2-b]pyridazine; Imidazo[4,5-b]pyridine; Dual specificity tyrosine-phosphorylation-regulated kinase (DYRKs); Cyclin-dependent kinase (CDKs); Unicellular parasite; Alzheimer’s disease; Down syndrome; 615.19

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Bendjeddou, L. (2014). Synthèse et évaluation biologique de nouveaux inhibiteurs de kinases : identification d‘inhibiteurs de kinases parasitaires : Synthesis and biological evaluation of new kinase inhibitors : identification of inhibitors of several parasite protein kinases. (Doctoral Dissertation). Université Paris Descartes – Paris V. Retrieved from http://www.theses.fr/2014PA05P615

Chicago Manual of Style (16^th Edition):

Bendjeddou, Lyamin. “Synthèse et évaluation biologique de nouveaux inhibiteurs de kinases : identification d‘inhibiteurs de kinases parasitaires : Synthesis and biological evaluation of new kinase inhibitors : identification of inhibitors of several parasite protein kinases.” 2014. Doctoral Dissertation, Université Paris Descartes – Paris V. Accessed January 26, 2021. http://www.theses.fr/2014PA05P615.

MLA Handbook (7^th Edition):

Bendjeddou, Lyamin. “Synthèse et évaluation biologique de nouveaux inhibiteurs de kinases : identification d‘inhibiteurs de kinases parasitaires : Synthesis and biological evaluation of new kinase inhibitors : identification of inhibitors of several parasite protein kinases.” 2014. Web. 26 Jan 2021.

Vancouver:

Bendjeddou L. Synthèse et évaluation biologique de nouveaux inhibiteurs de kinases : identification d‘inhibiteurs de kinases parasitaires : Synthesis and biological evaluation of new kinase inhibitors : identification of inhibitors of several parasite protein kinases. [Internet] [Doctoral dissertation]. Université Paris Descartes – Paris V; 2014. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2014PA05P615.

Council of Science Editors:

Bendjeddou L. Synthèse et évaluation biologique de nouveaux inhibiteurs de kinases : identification d‘inhibiteurs de kinases parasitaires : Synthesis and biological evaluation of new kinase inhibitors : identification of inhibitors of several parasite protein kinases. [Doctoral Dissertation]. Université Paris Descartes – Paris V; 2014. Available from: http://www.theses.fr/2014PA05P615

Loughborough University

21. Fernandez, Beatriz. New functionalisation chemistry of 2- and 4-pyridones and related heterocycles.

Degree: PhD, 2016, Loughborough University

URL: http://hdl.handle.net/2134/21685

► New methodology for the synthesis of several 4H-pyrido[1,2-a]pyrimidin-4-ones has been developed from commercially available 2-aminopyridines and β-oxo esters catalysed by Montmorillonite under solvent-free conditions in… (more)

Subjects/Keywords: 547; Pyridone; Quinolizinone; 4H-pyrido[1]; 2-[a]pyrimidin-4-ones; 4H-pyrimido[1]; 2-[a]pyrimidin-4-one

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Fernandez, B. (2016). New functionalisation chemistry of 2- and 4-pyridones and related heterocycles. (Doctoral Dissertation). Loughborough University. Retrieved from http://hdl.handle.net/2134/21685

Chicago Manual of Style (16^th Edition):

Fernandez, Beatriz. “New functionalisation chemistry of 2- and 4-pyridones and related heterocycles.” 2016. Doctoral Dissertation, Loughborough University. Accessed January 26, 2021. http://hdl.handle.net/2134/21685.

MLA Handbook (7^th Edition):

Fernandez, Beatriz. “New functionalisation chemistry of 2- and 4-pyridones and related heterocycles.” 2016. Web. 26 Jan 2021.

Vancouver:

Fernandez B. New functionalisation chemistry of 2- and 4-pyridones and related heterocycles. [Internet] [Doctoral dissertation]. Loughborough University; 2016. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/2134/21685.

Council of Science Editors:

Fernandez B. New functionalisation chemistry of 2- and 4-pyridones and related heterocycles. [Doctoral Dissertation]. Loughborough University; 2016. Available from: http://hdl.handle.net/2134/21685

22. Ruiz Ortiz, Fernando María. Vida humana y luz de la palabra.

Degree: Departament d'Humanitats, 2016, Universitat Abat Oliba CEU

URL: http://hdl.handle.net/10803/399535

► The word of the man, sign by excellence of human communication, has been considered philosophers since the so called “lingüístic turn” as something which is… (more)

Subjects/Keywords: 1; 2

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Ruiz Ortiz, F. M. (2016). Vida humana y luz de la palabra. (Thesis). Universitat Abat Oliba CEU. Retrieved from http://hdl.handle.net/10803/399535

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Ruiz Ortiz, Fernando María. “Vida humana y luz de la palabra.” 2016. Thesis, Universitat Abat Oliba CEU. Accessed January 26, 2021. http://hdl.handle.net/10803/399535.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Ruiz Ortiz, Fernando María. “Vida humana y luz de la palabra.” 2016. Web. 26 Jan 2021.

Vancouver:

Ruiz Ortiz FM. Vida humana y luz de la palabra. [Internet] [Thesis]. Universitat Abat Oliba CEU; 2016. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/10803/399535.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Ruiz Ortiz FM. Vida humana y luz de la palabra. [Thesis]. Universitat Abat Oliba CEU; 2016. Available from: http://hdl.handle.net/10803/399535

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

23. Elie, Jonathan. Développement de médicaments radiopharmaceutiques fluorés pour l'exploration en imagerie moléculaire TEP de la neuroinflammation : Fluorinated radiopharmaceuticals drug development for the exploration of neuroinflammation by PET molecular imaging.

Degree: Docteur es, Sciences de la Vie et de la Santé, 2016, Université François-Rabelais de Tours

URL: http://www.theses.fr/2016TOUR3302

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Les maladies du système nerveux central (SNC) comme la sclérose en plaques, les accidents vasculaires cérébraux et les maladies neurodégénératives (Alzheimer et Parkinson) entraînent une… (more)

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Les maladies du système nerveux central (SNC) comme la sclérose en plaques, les accidents vasculaires cérébraux et les maladies neurodégénératives (Alzheimer et Parkinson) entraînent une réponse inflammatoire au niveau cérébrale appelée neuroinflammation. Ce phénomène peut avoir pour conséquence la limitation de la propagation de la maladie mais aussi la réparation et la régénération des tissus touchés. La microglie, principale défense du SNC, passe à un stade activé lors de phénomènes neuroinflammatoires et va libérer de nombreux facteurs neuroprotecteurs mais aussi pro-inflammatoires. Cette dualité d’action va ainsi maintenir un cercle vicieux, pouvant conduire à la mort neuronale. Il serait donc intéressant de comprendre le mécanisme de la neuroinflammation pour diagnostiquer et traiter au mieux les pathologies du SNC. Il existe plusieurs cibles moléculaires, parmi elles se trouvent la CycloOXygénase 2 (COX-2), une enzyme qui permet la formation de prostaglandines à partir de l'acide arachidonique, qui apparaît précocement et est fortement surexprimée en cas de neuroinflammation. Cette enzyme serait donc une cible de choix pour le développement d’outils d’imagerie dans le but de diagnostiquer les pathologies dans lesquelles les processus inflammatoires centraux sont présents et ce afin d’améliorer la prise en charge du patient. La tomographie d’émission de positons (TEP) est une technique d’imagerie fonctionnelle très sensible qui permet de quantifier de manière fine les variations d’activités métaboliques ou moléculaires. Cette technique requiert l’utilisation de radiotraceurs marqués avec un émetteur béta+.

Central nervous system (CNS) disorders as multiple sclerosis, stroke and neurodegenerative diseases (Alzheimer’s and Parkinson’s) lead to inflammatory response in the brain called neuroinflammation. This phenomenon usually should result in limiting the spread of the disease but also repair and regeneration of the affected tissues. Microglia, the main defense of the SNC, which is activated during a neurodegenerative event leading to the production of many factors including neuroprotectors but also pro-inflammatories. This duality of actions will thereby maintain endless vicious circle leading to neuronal death. It would be interesting to understand the neuroinflammation mechanism to better diagnose and treat CNS diseases. There are several molecular targets, among them are the CycloOXygenase 2 (COX-2), an enzyme which allows the formation of prostaglandins from arachidonic acid, which appears early and it is significantly overexpressed in case of neuroinflammation. This enzyme is therefore a good biological target for the development of imaging tools in order to diagnose pathologies in which central inflammatory processes are present in order to improve patient care. Postiron emission tomography (PET) is a very sensitive functional imaging technique that quantifies minute variations in metabolic or molecular activities. This technique requires the use of radiotracers labeled with a beta + emitter.

Advisors/Committee Members: Vercouillie, Johnny (thesis director).

Subjects/Keywords: Neuroinflammation; AINS; COX-2; Radiomarquage; TEP; Iodonium; (aza)indazole; Imidazo[2,1-b][1,2,3]thiadiazole; Neuroinflammation; NSAID; COX-2; Radiolabeling; PET; Iodonium; (aza)indazole; Imidazo[2,1-b][1,2,3]thiadiazole

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Elie, J. (2016). Développement de médicaments radiopharmaceutiques fluorés pour l'exploration en imagerie moléculaire TEP de la neuroinflammation : Fluorinated radiopharmaceuticals drug development for the exploration of neuroinflammation by PET molecular imaging. (Doctoral Dissertation). Université François-Rabelais de Tours. Retrieved from http://www.theses.fr/2016TOUR3302

Chicago Manual of Style (16^th Edition):

Elie, Jonathan. “Développement de médicaments radiopharmaceutiques fluorés pour l'exploration en imagerie moléculaire TEP de la neuroinflammation : Fluorinated radiopharmaceuticals drug development for the exploration of neuroinflammation by PET molecular imaging.” 2016. Doctoral Dissertation, Université François-Rabelais de Tours. Accessed January 26, 2021. http://www.theses.fr/2016TOUR3302.

MLA Handbook (7^th Edition):

Elie, Jonathan. “Développement de médicaments radiopharmaceutiques fluorés pour l'exploration en imagerie moléculaire TEP de la neuroinflammation : Fluorinated radiopharmaceuticals drug development for the exploration of neuroinflammation by PET molecular imaging.” 2016. Web. 26 Jan 2021.

Vancouver:

Elie J. Développement de médicaments radiopharmaceutiques fluorés pour l'exploration en imagerie moléculaire TEP de la neuroinflammation : Fluorinated radiopharmaceuticals drug development for the exploration of neuroinflammation by PET molecular imaging. [Internet] [Doctoral dissertation]. Université François-Rabelais de Tours; 2016. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2016TOUR3302.

Council of Science Editors:

Elie J. Développement de médicaments radiopharmaceutiques fluorés pour l'exploration en imagerie moléculaire TEP de la neuroinflammation : Fluorinated radiopharmaceuticals drug development for the exploration of neuroinflammation by PET molecular imaging. [Doctoral Dissertation]. Université François-Rabelais de Tours; 2016. Available from: http://www.theses.fr/2016TOUR3302

Universidade Estadual de Campinas

24. Alves, Brunna Eulálio, 1979-. Avaliação de moduladores do aumento da permeabilidade microvascular e sua correlação com a evolução clínica na sepse em pacientes onco-hematológicos neutropênicos febris: Evoluation of modulators of increased microvascular permeability and its correlation with clinical outcome in sepsis in patients with hematologic malignancies and febrile neutropenia.

Degree: 2011, Universidade Estadual de Campinas

URL: http://repositorio.unicamp.br/jspui/handle/REPOSIP/309168

► Abstract: Patients with hematologic malignancy and neutropenia represent a group at high risk of sepsis and septic shock. In recent decades, target-specific therapeutic strategies for… (more)

▼ Abstract: Patients with hematologic malignancy and neutropenia represent a group at high risk of sepsis and septic shock. In recent decades, target-specific therapeutic strategies for sepsis did not change significantly the survival of patients and treatment is still based on antibiotic therapy and supportive care, with high mortality rates. The breakdown of the endothelial barrier is a key event in the pathophysiology of septic shock and understanding of the mechanisms involved in this event has the potential to assist in the identification of new biomarkers and severity of new therapeutic targets for these patients. Recent studies have demonstrated the involvement of endothelial growth factor (VEGF-A), its soluble receptor (sFlt-1) and angiopoietins 1 and 2, proteins involved in angiogenesis and in regulation of endothelial barrier integrity in the pathogenesis of shock septic patients without cancer admitted to the intensive care unit. In this study, we prospectively evaluated the kinetics of VEGF-A, sFlt-1 and angiopoietins 1 and 2 during the initial 48 hours of febrile neutropenia in 41 patients with hematological malignancy undergoing intensive chemotherapy or conditioning regimen for stem cell transplantation hematopoietic cells by the same dosage by enzyme immunoassay. We also explored the association of serum levels of these biomarkers with the severity of sepsis through correlation with the MASCC, an index developed to identify patients with febrile neutropenia at low risk, and the SOFA score for assessment of organ dysfunction in patients with sepsis, both widely accepted. Progression to septic shock was associated with significantly higher levels of VEGF-A, sFlt-1 and angiopoietin-2 48 hours after the onset of febrile neutropenia when compared to values in patients with uncomplicated sepsis and the estimation of diagnostic accuracy suggests the ability to discriminate among patients who developed septic shock. These biomarkers also correlated with the severity scores, suggesting the biological relevance of the association Advisors/Committee Members: UNIVERSIDADE ESTADUAL DE CAMPINAS (CRUESP), Paula, Erich Vinicius de, 1972- (advisor), Universidade Estadual de Campinas. Faculdade de Ciências Médicas (institution), Programa de Pós-Graduação em Clínica Médica (nameofprogram), Neto, Abrahão Elias Hallack (committee member), Morelli, Vania Maris (committee member), Vigorito, Afonso Celso (committee member), Gilli, Simone Cristina Olenscki (committee member).

Subjects/Keywords: Sepse; Neutropenia; Fator A de crescimento do endotélio; Angiopoietina-1; Angiopoietina-2; Sepsis; Neutropenia; Vascular Endothelial Growth Factor A; Angiopoietin-1; Angiopoietin-2

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Alves, Brunna Eulálio, 1. (2011). Avaliação de moduladores do aumento da permeabilidade microvascular e sua correlação com a evolução clínica na sepse em pacientes onco-hematológicos neutropênicos febris: Evoluation of modulators of increased microvascular permeability and its correlation with clinical outcome in sepsis in patients with hematologic malignancies and febrile neutropenia. (Thesis). Universidade Estadual de Campinas. Retrieved from http://repositorio.unicamp.br/jspui/handle/REPOSIP/309168

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Alves, Brunna Eulálio, 1979-. “Avaliação de moduladores do aumento da permeabilidade microvascular e sua correlação com a evolução clínica na sepse em pacientes onco-hematológicos neutropênicos febris: Evoluation of modulators of increased microvascular permeability and its correlation with clinical outcome in sepsis in patients with hematologic malignancies and febrile neutropenia.” 2011. Thesis, Universidade Estadual de Campinas. Accessed January 26, 2021. http://repositorio.unicamp.br/jspui/handle/REPOSIP/309168.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Alves, Brunna Eulálio, 1979-. “Avaliação de moduladores do aumento da permeabilidade microvascular e sua correlação com a evolução clínica na sepse em pacientes onco-hematológicos neutropênicos febris: Evoluation of modulators of increased microvascular permeability and its correlation with clinical outcome in sepsis in patients with hematologic malignancies and febrile neutropenia.” 2011. Web. 26 Jan 2021.

Vancouver:

Alves, Brunna Eulálio 1. Avaliação de moduladores do aumento da permeabilidade microvascular e sua correlação com a evolução clínica na sepse em pacientes onco-hematológicos neutropênicos febris: Evoluation of modulators of increased microvascular permeability and its correlation with clinical outcome in sepsis in patients with hematologic malignancies and febrile neutropenia. [Internet] [Thesis]. Universidade Estadual de Campinas; 2011. [cited 2021 Jan 26]. Available from: http://repositorio.unicamp.br/jspui/handle/REPOSIP/309168.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Alves, Brunna Eulálio 1. Avaliação de moduladores do aumento da permeabilidade microvascular e sua correlação com a evolução clínica na sepse em pacientes onco-hematológicos neutropênicos febris: Evoluation of modulators of increased microvascular permeability and its correlation with clinical outcome in sepsis in patients with hematologic malignancies and febrile neutropenia. [Thesis]. Universidade Estadual de Campinas; 2011. Available from: http://repositorio.unicamp.br/jspui/handle/REPOSIP/309168

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

25. Abou samra, Alma. Conception, synthèse et évaluation biologique d’inhibiteurs des protéines anti-apoptotiques de la famille Bcl-2 : Development and biological evaluation of small molecules inhibitors of anti-apoptotic proteins of Bcl-2 family.

Degree: Docteur es, Chimie thérapeutique, 2017, Université Paris-Saclay (ComUE)

URL: http://www.theses.fr/2017SACLS390

►

La mitochondrie joue un rôle capital dans la mort cellulaire programmée ou apoptose par l’intermédiaire des protéines de la famille Bcl-2. Le dérèglement de l'apoptose… (more)

▼

La mitochondrie joue un rôle capital dans la mort cellulaire programmée ou apoptose par l’intermédiaire des protéines de la famille Bcl-2. Le dérèglement de l'apoptose dans de nombreux cancers fait de cette voie et des protéines de la famille Bcl-2 des cibles prometteuses pour la thérapie anti-cancéreuse. Le développement de petites molécules ciblant les protéines de la famille Bcl-2 s’est toutefois révélé être un grand défi, et peu d’entre elles ont atteint des études de phase clinique. Cependant, depuis une quinzaine d’années, grâce à des approches variées et souvent innovantes, des composés très actifs ont été développés. Plusieurs composés sont actuellement en essais clinique et une molécule, le venetoclax, a obtenu la première autorisation de mise sur le marché en avril 2016. Ce succès thérapeutique démontre que les protéines de la famille de Bcl-2 sont des cibles potentielles pour la thérapie anticancéreuse.Les substances naturelles sont une source importante de nouvelles molécules à structures originales, et de nombreux médicaments utilisés actuellement en chimiothérapie sont d’origine naturelle. La meiogynine A est un triterpène dimère qui a été isolé et synthétisé dans notre équipe. Ce composé possède une activité inhibitrice duale des protéines anti-apoptotiques Bcl-xL et Mcl-1. Des analogues de première et deuxième génération ont été élaborés par la suite, parmi lesquels, certains présentent une activité duale sub-micromolaire. Contrairement aux analogues de première génération, ces composés ne sont cependant pas cytotoxiques, probablement en raison de la présence d’une fonction ester sur la chaine latérale qui peut s’hydrolyser en un métabolite inactif.Mon projet de thèse vise à élaborer des analogues de troisième génération de la meiogynine A possédant une activité inhibitrice multiple sub-micromolaire des protéines anti-apoptotiques Bcl-xL, Mcl-1, Bcl-2 et cytotoxiques sur des lignées cellulaires surexprimant ces mêmes protéines. Pour cela, un essai biologique de mesure d’inhibition de l’interaction Bcl-2/Bim a été mis en place et robotisé afin d’évaluer l’activité biologique des composés synthétisés. De plus, la voie de synthèse bioinspirée d’un précurseur commun des nouveaux analogues a été mise au point à l’échelle de plusieurs grammes. Ce précurseur a permis d’élaborer différents analogues de troisième génération de la meiogynine A en réalisant des pharmacomodulations sur la chaîne latérale afin de remplacer la fonction ester des analogues de deuxième génération par un groupement stable et résistant in cellulo. Différentes séries ont été envisagées (alcènes, amines, amides, carbamates et triazoles). L’activité biologique des composés synthétisés a été évaluée sur les trois cibles in vitro. Finalement, des analyses de cytotoxicité pour les analogues les plus actifs ont été réalisées par nos collaborateurs à l’Institut Gustave Roussy.

Apoptosis is used by multicellular organisms to regulate tissue homeostasis through the elimination of useless or potentially harmful cells. The key players of…

Advisors/Committee Members: Roussi, Fanny (thesis director).

Subjects/Keywords: Apoptose; Inhibiteurs multiples; Bcl-2; Bcl-XL; Mcl-1; Meiogynine A; Apoptosis; Multiple inhibitors; Bcl-2; Bcl-XL; Mcl-1; Meiogynine A

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Abou samra, A. (2017). Conception, synthèse et évaluation biologique d’inhibiteurs des protéines anti-apoptotiques de la famille Bcl-2 : Development and biological evaluation of small molecules inhibitors of anti-apoptotic proteins of Bcl-2 family. (Doctoral Dissertation). Université Paris-Saclay (ComUE). Retrieved from http://www.theses.fr/2017SACLS390

Chicago Manual of Style (16^th Edition):

Abou samra, Alma. “Conception, synthèse et évaluation biologique d’inhibiteurs des protéines anti-apoptotiques de la famille Bcl-2 : Development and biological evaluation of small molecules inhibitors of anti-apoptotic proteins of Bcl-2 family.” 2017. Doctoral Dissertation, Université Paris-Saclay (ComUE). Accessed January 26, 2021. http://www.theses.fr/2017SACLS390.

MLA Handbook (7^th Edition):

Abou samra, Alma. “Conception, synthèse et évaluation biologique d’inhibiteurs des protéines anti-apoptotiques de la famille Bcl-2 : Development and biological evaluation of small molecules inhibitors of anti-apoptotic proteins of Bcl-2 family.” 2017. Web. 26 Jan 2021.

Vancouver:

Abou samra A. Conception, synthèse et évaluation biologique d’inhibiteurs des protéines anti-apoptotiques de la famille Bcl-2 : Development and biological evaluation of small molecules inhibitors of anti-apoptotic proteins of Bcl-2 family. [Internet] [Doctoral dissertation]. Université Paris-Saclay (ComUE); 2017. [cited 2021 Jan 26]. Available from: http://www.theses.fr/2017SACLS390.

Council of Science Editors:

Abou samra A. Conception, synthèse et évaluation biologique d’inhibiteurs des protéines anti-apoptotiques de la famille Bcl-2 : Development and biological evaluation of small molecules inhibitors of anti-apoptotic proteins of Bcl-2 family. [Doctoral Dissertation]. Université Paris-Saclay (ComUE); 2017. Available from: http://www.theses.fr/2017SACLS390

Universidade do Rio Grande do Sul

26. Zanatta, Claudete Maria. Avaliação do sistema endotelina na nefropatia diabética em pacientes com diabete melito tipo 2.

Degree: 2009, Universidade do Rio Grande do Sul

URL: http://hdl.handle.net/10183/21440

► Introdução: A nefropatia diabética (ND) é uma das principais complicações crônicas do diabete melito (DM), sendo que cerca de 25 a 40% dos pacientes com… (more)

▼ Introdução: A nefropatia diabética (ND) é uma das principais complicações crônicas do diabete melito (DM), sendo que cerca de 25 a 40% dos pacientes com DM tipo 1 e 20 a 50% dos pacientes com DM tipo 2 desenvolvem ND ao longo da vida, dependendo da origem étnica. Estudos de agregação familiar mostram uma importante concordância para o desenvolvimento de ND em algumas famílias e reforçam a hipótese de que existem fatores genéticos envolvidos na sua patogênese. O sistema endotelina tem sido relacionado na patogênese da hipertensão arterial e desordens renais. A endotelina-1 (ET-1) regula a vasoconstrição e proliferação celular nos tecidos através da ativação do receptor tipo A (ETRA). Em tecidos de rins normais, ET-1 e ETRA estão mais expressos em vasos e em menor intensidade no glomérulo. Em modelos animais com DM, a expressão de ET-1 é cinco vezes maior, sugerindo uma potencial associação entre o sistema endotelina e ND. No presente estudo, avaliamos a associação de polimorfismos do gene da ET-1 (EDN1) e ETRA (EDNRA) com a ND em pacientes com DM tipo 2 e a expressão da ET-1 e ETRA em biópsias de rins de pacientes com ND, Nefropatia por IgA e tecido de rins normais. Materiais e Métodos: O estudo de genética, um estudo caso controle a partir de um estudo transversal, com 548 pacientes brancos com DM tipo 2. Os casos foram considerados pacientes com proteinúria (excreção urinária de albumina (EUA) > 200 mg/min ou 174 mg/24h, em coleta de 24h ou em amostra de urina respectivamente) ou em diálise e controles pacientes com normoalbuminúria (EUA < 20mg/min ou < 17 mg/l) e DM tipo 2 por mais de 5 anos. Foram genotipados dois polimorfismos (SNP) do gene da EDN1 (rs1800541 or T- 1370G; rs57072783 or Lys198Asn) e cinco do gene do EDNRA (rs6842241; rs4835083; rs4639051; rs5333 and rs5343). A análise de haplótipos foi realizada através do programa PHASE versão 2.1. A frequência dos alelos, genótipos e haplótipos foi comparada entre casos e controles. O equilíbrio de Hardy-Weinberg de cada SNP foi testado através do teste do c² de Pearson. No estudo de imunohistoquimica, analisamos a expressão da ET-1 e ETRA em treze biópsias de pacientes com DM tipo 2 e ND, dez biópsias de pacientes proteinúricos por Nefropatia por IgA e treze amostras de tecido de rim normal que realizaram nefrectomia por tumor. Resultados: Considerando um modelo dominante, a presença do alelo T do rs57072783 (TT/TG vs. GG) foi protetor contra DN (OR = 0.69; IC 95% 0.48-0.99, P = 0.049), enquanto a presença do alelo G do rs1800541 (GG/GT vs. TT) foi associado com OR = 0.60 (IC 95% 0.41-0.88, P=0.009). Entretanto na análise multivariada, somente o genótipo GG/GT do rs1800541 permaneceu com associação independente com a ND (P = 0.046). A expressão da ET-1 em biópsias de pacientes com ND e Nefropatia por IgA estava aumentada nas células endoteliais de capilares glomerulares e capilares peri tubulares quando comparado com controles (P = 0,001). A expressão do ETRA também foi mais intensa na ND e Nefropatia por IgA em relação aos controles (P = 0,019). Pacientes… Advisors/Committee Members: Canani, Luis Henrique Santos.

Subjects/Keywords: Diabetes mellitus tipo 2; Nefropatias diabéticas; Polimorfismo genético; Endotelina-1; Receptor de endotelina A

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Zanatta, C. M. (2009). Avaliação do sistema endotelina na nefropatia diabética em pacientes com diabete melito tipo 2. (Thesis). Universidade do Rio Grande do Sul. Retrieved from http://hdl.handle.net/10183/21440

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Zanatta, Claudete Maria. “Avaliação do sistema endotelina na nefropatia diabética em pacientes com diabete melito tipo 2.” 2009. Thesis, Universidade do Rio Grande do Sul. Accessed January 26, 2021. http://hdl.handle.net/10183/21440.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Zanatta, Claudete Maria. “Avaliação do sistema endotelina na nefropatia diabética em pacientes com diabete melito tipo 2.” 2009. Web. 26 Jan 2021.

Vancouver:

Zanatta CM. Avaliação do sistema endotelina na nefropatia diabética em pacientes com diabete melito tipo 2. [Internet] [Thesis]. Universidade do Rio Grande do Sul; 2009. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/10183/21440.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Zanatta CM. Avaliação do sistema endotelina na nefropatia diabética em pacientes com diabete melito tipo 2. [Thesis]. Universidade do Rio Grande do Sul; 2009. Available from: http://hdl.handle.net/10183/21440

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

27. Raquel Bicudo Mendonça. Teste de provocação oral aberto na confirmação de alergia ao leite de vaca mediada por imunoglobulina E.

Degree: 2010, Universidade Federal de São Paulo

URL: http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=511

► Objetivo: Descrever o teste de provocação oral aberto aplicado a crianças menores de três anos de idade com suspeita ou diagnóstico prévio de alergia ao… (more)

▼ Objetivo: Descrever o teste de provocação oral aberto aplicado a crianças menores de três anos de idade com suspeita ou diagnóstico prévio de alergia ao leite de vaca mediada por imunoglobulinas E. Relacionar a história clínica e o resultado do teste cutâneo com o resultado do teste de provocação oral. Métodos: Crianças com idades entre cinco e 36 meses, selecionadas de acordo com a história sugestiva de reações imediatas à ingestão de leite de vaca, com teste cutâneo positivo para leite de vaca e/ou suas frações protéicas, foram submetidas ao teste de provocação oral aberto com 100 mL de leite de vaca, oferecidos em doses progressivas (1, 4, 10, 15, 20, 25 e 25 mL) em intervalos de 15 a 20 minutos, seguido por período de observação de duas horas. O teste foi realizado em ambiente hospitalar, por especialistas. Resultados: Foram avaliadas 46 crianças (mediana de idade 13,8 meses), das quais 41,3% tiveram resultado positivo. Os principais sintomas observados nas crianças com teste de provocação oral positivo foram os cutâneos (73,7%), seguidos pelos respiratórios (57,9%) e gastrintestinais (36,8%). De acordo com a gravidade das reações, 57,9%, 36,8% e 5,3% dessas crianças apresentaram reações leves, moderadas e graves, respectivamente. O uso de anti-histamínico oral foi suficiente para remissão dos sinais e sintomas, em todos os casos positivos. Em relação ao intervalo entre a ingestão de leite de vaca e o aparecimento de reações, 68,4% das crianças com teste de provocação oral positivo apresentaram reações nos primeiros 20 minutos de teste. Para a maioria delas (63,2%) a ingestão de 1 mL de leite de vaca foi suficiente para deflagrar reações. Observou-se maior freqüência de teste cutâneo positivo para leite de vaca total e caseína nas crianças com teste de provocação oral positivo, com diferença estatisticamente significante em relação aquelas com teste de provocação oral negativo. Conclusões: O método demonstrou-se adequado a crianças com até três anos de idade, seguro e de fácil execução. Houve concordância significante entre as reações relatadas pela família na história clínica e as observadas durante o teste de provocação oral, para crianças que tiveram resultado positivo. A positividade ao teste cutâneo com leite de vaca total e caseína apresentou associação significante com a positividade ao teste de provocação oral. Advisors/Committee Members: Dirceu Solé, Neusa Falbo Wandalsen, Maria Elisabeth Machado Pinto e Silva, Fernanda Cobayashi.

Subjects/Keywords: 1. Hipersensibilidade Alimentar/diagnóstico. 2. Hipersensibilidade a Leite/diagnóstico. 3. Lactente. 4. Pré-Escolar.; PEDIATRIA

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Mendonça, R. B. (2010). Teste de provocação oral aberto na confirmação de alergia ao leite de vaca mediada por imunoglobulina E. (Thesis). Universidade Federal de São Paulo. Retrieved from http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=511

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Mendonça, Raquel Bicudo. “Teste de provocação oral aberto na confirmação de alergia ao leite de vaca mediada por imunoglobulina E.” 2010. Thesis, Universidade Federal de São Paulo. Accessed January 26, 2021. http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=511.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Mendonça, Raquel Bicudo. “Teste de provocação oral aberto na confirmação de alergia ao leite de vaca mediada por imunoglobulina E.” 2010. Web. 26 Jan 2021.

Vancouver:

Mendonça RB. Teste de provocação oral aberto na confirmação de alergia ao leite de vaca mediada por imunoglobulina E. [Internet] [Thesis]. Universidade Federal de São Paulo; 2010. [cited 2021 Jan 26]. Available from: http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=511.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Mendonça RB. Teste de provocação oral aberto na confirmação de alergia ao leite de vaca mediada por imunoglobulina E. [Thesis]. Universidade Federal de São Paulo; 2010. Available from: http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=511

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

28. Leonardo Reichmann Fasolo. Topografia de papila, análise da camada de fibras nervosas da retina e perimetrias azul-amarelo e de freqüência duplicada no glaucoma.

Degree: 2005, Universidade Federal de São Paulo

URL: http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=69

► Introdução: Comparar o tomógrafo retiniano de Heidelberg (HRT II), analisador da camada de fibras nervosas (GDx), perimetria azul-amarelo (PAA) e perimetria de freqüência duplicada (FDT)… (more)

▼ Introdução: Comparar o tomógrafo retiniano de Heidelberg (HRT II), analisador da camada de fibras nervosas (GDx), perimetria azul-amarelo (PAA) e perimetria de freqüência duplicada (FDT) no diagnóstico do glaucoma individualmente, assim como em conjunto. Métodos: Sessenta portadores de glaucoma primário de ângulo aberto e 60 normais foram submetidos a exames de HRT, GDx, PAA e FDT. Sensibilidade, especificidade, área sob a curva ROC e análise de regressão logística foram realizados entre as tecnologias. Significância estatística foi determinada com 95%. Resultados: O melhor índice do HRT foi o parâmetro LCDR com a maior área sob a curva ROC (0,89), que foi superior ao mean deviation (MD) da PAA (0,81), ao the number do GDx (0,80) e ao MD do FDT (0,78). Quando foram estudadas as tecnologias isoladamente, a análise de regressão logística apresentou melhores índices de razão das chances para glaucoma com exames positivos para o HRT (22,49), seguido pela PAA (21,71). FDT(3,97) e GDx (2,73). Quando se associaram exames positivos de diferentes tecnologias, as razões das chances aumentaram. Nos casos com exames de HRT, FDT e PAA fora dos limites normais, a razão das chances foi de 252,6 e com HRT, PAA e GDx alterados, 173,1. Com todos os exames fora dos limites normais, a razão das chances de ter glaucoma evoliu a 689,7. O comportamento da sensibilidade das diferentes tecnologias em função da gravidade do glaucoma foi medido através do MD da perimetria automatizada acromática. Nos pacientes com MD de 5 dB, a sensibilidade do HRT foi de 44%, do FDT de 67,9%, da PAA de 47,9% e do GDx de 63,2%. Naqueles com MD de 15 dB, a sensibilidade dos aparelhos foi a 77,8%, 97,5%, 97,2% e 76,2%, respectivamente. À medida que o MD foi diminuindo, o que é compatível com glaucomas mais avançados, a sensibilidade de todos os aparelhos melhorou. Quanto à evolução da especificidade em função do MD da perimetria automatizada acromática. O HRT, o PAA e o FDT apresentaram piora de especificidade em relação à diminuição do MD, ao contrário do GDx, que apresentou melhora. Conclusão: O HRT, representado pelo parâmetro LCDR apresentou melhor capacidade de diferenciar normais de glaucomatosos entre os aparelhos estudados. A análise de regressão logística confirmou que a presença de exames alterados de HRT ou PAA apresentam as maiores razões das chances de glaucoma. A associação de exames alterados aumentou a razão das chances, principalmente, quando o HRT e a PAA estavam fora dos limites normais. Uma melhora da sensibilidade de todas as tecnologias foi obtida na mesma proporção em que o MD da perimetria acromática foi diminuindo. Entretanto, baixos níveis de sensibilidade foram obtidos em pacientes com MD de 5 dB, o que demonstra uma deficiência destes aparelhos em diagnosticar os casos com glaucoma em estádios mais precoces da doença. Advisors/Committee Members: João Antonio Prata Junior, Augusto Paranhos Junior, Carmo Mandia Júnior.

Subjects/Keywords: 1.Polarimetria de varredura a laser; 2.Perimetria; 3.Glaucoma; 4.Oftalmoscopia confocal; OFTALMOLOGIA

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APA (6^th Edition):

Fasolo, L. R. (2005). Topografia de papila, análise da camada de fibras nervosas da retina e perimetrias azul-amarelo e de freqüência duplicada no glaucoma. (Thesis). Universidade Federal de São Paulo. Retrieved from http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=69

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Fasolo, Leonardo Reichmann. “Topografia de papila, análise da camada de fibras nervosas da retina e perimetrias azul-amarelo e de freqüência duplicada no glaucoma.” 2005. Thesis, Universidade Federal de São Paulo. Accessed January 26, 2021. http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=69.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Fasolo, Leonardo Reichmann. “Topografia de papila, análise da camada de fibras nervosas da retina e perimetrias azul-amarelo e de freqüência duplicada no glaucoma.” 2005. Web. 26 Jan 2021.

Vancouver:

Fasolo LR. Topografia de papila, análise da camada de fibras nervosas da retina e perimetrias azul-amarelo e de freqüência duplicada no glaucoma. [Internet] [Thesis]. Universidade Federal de São Paulo; 2005. [cited 2021 Jan 26]. Available from: http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=69.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Fasolo LR. Topografia de papila, análise da camada de fibras nervosas da retina e perimetrias azul-amarelo e de freqüência duplicada no glaucoma. [Thesis]. Universidade Federal de São Paulo; 2005. Available from: http://www.bdtd.unifesp.br/tede//tde_busca/arquivo.php?codArquivo=69

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

29. Yuan, Changxia. Synthesis of complanadine A and phthaloyl peroxide-mediated oxidations of alkenes and arenes.

Degree: PhD, Chemistry, 2013, University of Texas – Austin

URL: http://hdl.handle.net/2152/46250

► The natural product complanadine A has shown promise in regenerative science, promoting neuronal outgrowth by inducing the secretion of growth factors from glial cells. Through… (more)

▼ The natural product complanadine A has shown promise in regenerative science, promoting neuronal outgrowth by inducing the secretion of growth factors from glial cells. Through the use of tandem, cobalt-mediated [2+2+2] cycloaddition reactions two synthetic routes have been developed with different sequences for the formation of the unsymmetric bipyridyl core. The regioselective formation of each of the pyridines was achieved based on the inherent selectivity of the molecules or by reversing this inate regioselectivity through the addition of Lewis bases. This strategy has been successfully employed to provide laboratory access to complanadine A as well as structurally related compounds possessing the lycodine core. Phthaloyl peroxide derivatives have the potential to function as organocatalysts for the dihydroxylation of alkenes. The development of an organocatalytic system for the syn-dihydroxylation of alkenes, using hydrogen peroxide as the stoichiometric oxidant, could minimize the waste and cost associated with the current industrial process. With new access to phthaloyl peroxide derivatives, this dihydroxylation method was improved with stoichiometric dichlorophthaloyl peroxide for the dihydroxylation of alkenes. Substituted phenols are broadly useful compounds, functioning as starting materials and end products in all areas of chemical industry. Since the initial discovery of phenol from coal tar advances have been made in the synthetic preparations of this class of compounds which possess a hydroxyl group appended to an aromatic hydrocarbon core. Ideally the synthesis of phenols is achieved through the direct installation of oxygen into an aromatic precursor, which is typically more abundant. In this thesis it is discussed how phthaloyl peroxide, in the absence of other reagents, enables the conversion of aromatic hydrocarbons to phenols even when the precursors possess functionality that is incompatible with strongly oxidizing conditions. The reaction is shown to proceed through a "reverse rebound" mechanism as opposed to the classical rebound mechanism, providing insight into the unique aryl selectivity of the chemical transformation. Advisors/Committee Members: Siegel, Dionicio R. (advisor), Anslyn, Eric V. (committee member), Willson, Grant C. (committee member), Liu, Hung-Wen (committee member), Humphrey, Simon M. (committee member).

Subjects/Keywords: Complanadine A; [2+2+2]; Pyridine; Phthaloyl peroxide; Dihydroxylation; Hydroxylation; Reverse rebound mechanism

…xiv CHAPTER 1 Background for (–)-Complanadine A and (+)-Lycodine… …1 1.1 Isolation and Structural Characterization of Complanadine A… …2 1.2 Biological Activity of Complanadine A… …14 CHAPTER 2 Synthesis of Complanadine A and Lycodine - First and Second Generation… …2 Figure 1.2. NOE analysis of complanadine A (1.2)…

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Yuan, C. (2013). Synthesis of complanadine A and phthaloyl peroxide-mediated oxidations of alkenes and arenes. (Doctoral Dissertation). University of Texas – Austin. Retrieved from http://hdl.handle.net/2152/46250

Chicago Manual of Style (16^th Edition):

Yuan, Changxia. “Synthesis of complanadine A and phthaloyl peroxide-mediated oxidations of alkenes and arenes.” 2013. Doctoral Dissertation, University of Texas – Austin. Accessed January 26, 2021. http://hdl.handle.net/2152/46250.

MLA Handbook (7^th Edition):

Yuan, Changxia. “Synthesis of complanadine A and phthaloyl peroxide-mediated oxidations of alkenes and arenes.” 2013. Web. 26 Jan 2021.

Vancouver:

Yuan C. Synthesis of complanadine A and phthaloyl peroxide-mediated oxidations of alkenes and arenes. [Internet] [Doctoral dissertation]. University of Texas – Austin; 2013. [cited 2021 Jan 26]. Available from: http://hdl.handle.net/2152/46250.

Council of Science Editors:

Yuan C. Synthesis of complanadine A and phthaloyl peroxide-mediated oxidations of alkenes and arenes. [Doctoral Dissertation]. University of Texas – Austin; 2013. Available from: http://hdl.handle.net/2152/46250

30. Rosenberg, Adam Jason. Development of Pd Catalyzed Amidations & Applications to the Synthesis of Heterocycles.

Degree: PhD, Chemistry, 2013, Syracuse University

URL: https://surface.syr.edu/etd/12

► Chapter 1 A brief overview of C-N amide bond formation: past methods and current catalytic approaches. Chapter 2 A facile synthesis of imidazo[4,5-b]pyridines and… (more)

Subjects/Keywords: Heterocycles; Imidazo[4; 5-b]pyridine; Imidazopyridine; Palladium; Pentosidine; Chemistry

…D. A. Org. Lett. 2012, 14(17), 4678461. “Synthesis of 2-amino-imidazo[4,5… …x28;Fig. 2) Alkylation of the unsubstituted imidazo[4,5-b]pyridine is… …was obtained in a 10:1 mixture, the reduced pyridine being the primary product. (… …1 2.0 SYNTHESIS PALLADIUM OF IMIDAZO[4,5-B]PYRIDINES CATALYZED AMIDATION… …17 3.0 SYNTHESIS OF 2-AMINO-IMIDAZO[4,5-B]PYRIDINES…

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Rosenberg, A. J. (2013). Development of Pd Catalyzed Amidations & Applications to the Synthesis of Heterocycles. (Doctoral Dissertation). Syracuse University. Retrieved from https://surface.syr.edu/etd/12

Chicago Manual of Style (16^th Edition):

Rosenberg, Adam Jason. “Development of Pd Catalyzed Amidations & Applications to the Synthesis of Heterocycles.” 2013. Doctoral Dissertation, Syracuse University. Accessed January 26, 2021. https://surface.syr.edu/etd/12.

MLA Handbook (7^th Edition):

Rosenberg, Adam Jason. “Development of Pd Catalyzed Amidations & Applications to the Synthesis of Heterocycles.” 2013. Web. 26 Jan 2021.

Vancouver:

Rosenberg AJ. Development of Pd Catalyzed Amidations & Applications to the Synthesis of Heterocycles. [Internet] [Doctoral dissertation]. Syracuse University; 2013. [cited 2021 Jan 26]. Available from: https://surface.syr.edu/etd/12.

Council of Science Editors:

Rosenberg AJ. Development of Pd Catalyzed Amidations & Applications to the Synthesis of Heterocycles. [Doctoral Dissertation]. Syracuse University; 2013. Available from: https://surface.syr.edu/etd/12

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