Advanced search options

Advanced Search Options 🞨

Browse by author name (“Author name starts with…”).

Find ETDs with:

in
/  
in
/  
in
/  
in

Written in Published in Earliest date Latest date

Sorted by

Results per page:

Sorted by: relevance · author · university · dateNew search

You searched for subject:(Nitroreductases). Showing records 1 – 2 of 2 total matches.

Search Limiters

Last 2 Years | English Only

No search limiters apply to these results.

▼ Search Limiters


IUPUI

1. Howe, Christopher Ryan. Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli.

Degree: 2020, IUPUI

Indiana University-Purdue University Indianapolis (IUPUI) Advisors/Committee Members: Johnson, Steven M., Hoang, Quyen Q., Meroueh, Samy O..

Subjects/Keywords: Pro-Drugs; GroEL/ES; Chaperone Proteins; Nitrofurans; Hydroxyquinolines; Nitroreductases; Inhibitors

Record DetailsSimilar RecordsGoogle PlusoneFacebookTwitterCiteULikeMendeleyreddit

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

APA (6th Edition):

Howe, C. R. (2020). Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli. (Thesis). IUPUI. Retrieved from http://hdl.handle.net/1805/22885

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

Chicago Manual of Style (16th Edition):

Howe, Christopher Ryan. “Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli.” 2020. Thesis, IUPUI. Accessed November 24, 2020. http://hdl.handle.net/1805/22885.

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

MLA Handbook (7th Edition):

Howe, Christopher Ryan. “Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli.” 2020. Web. 24 Nov 2020.

Vancouver:

Howe CR. Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli. [Internet] [Thesis]. IUPUI; 2020. [cited 2020 Nov 24]. Available from: http://hdl.handle.net/1805/22885.

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

Council of Science Editors:

Howe CR. Analogues of Nitrofuran Antibiotics are Potent GroEL/ES Pro-drug Inhibitors with Efficacy against Enterococcus Faecium, Staphylococcus Aureus, and Escherichia Coli. [Thesis]. IUPUI; 2020. Available from: http://hdl.handle.net/1805/22885

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

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

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

Record DetailsSimilar RecordsGoogle PlusoneFacebookTwitterCiteULikeMendeleyreddit

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

APA (6th 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 (16th 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 November 24, 2020. http://www.theses.fr/2018AIXM0275.

MLA Handbook (7th 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. 24 Nov 2020.

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 2020 Nov 24]. 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

.