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Universitat de Barcelona

1. Petit Roig, Elena. Bioconjugació de poliols i tiols amb agents antivírics.

Degree: Departament de Química Inorgànica i Orgànica, 2019, Universitat de Barcelona

HIV-1 is still one of the most serious problems of global public health, especially in third world countries. The most advanced stage of HIV infection is AIDS (acquired immunodeficiency syndrome). The present Doctoral Thesis describes our efforts in the synthesis of a new generation of microbicides (4th generation), which are conjugates of antiviral drugs to polymeric structures or scaffolds to achieve a topical agent with controlled absorption. Thus, after an introduction on AIDS and microbicides, Chapter 1 deals with the preparation of 14 analogues of BMS806, which could be biologically tested as entry inhibitors, concluding that the best candidates were the products substituted on position 7 of indole. Chapter 2 includes the preparation of more derivatives of BMS806, testing the Cu(I)-catalyzed [3+2] cycloaddition of the azides shown in Chapter 1. Also, several ligands have been synthesized to reduce the cytotoxicity of this reaction. The conditions for carrying out the [3+2] cycloaddition reaction with polar substrates such as βCD in aqueous media have been optimized. Within the click reactions, Chapter 3 presents the development of a bioortogonal method based on the simple conjugate additions of thiols to activated terminal triple bonds under physiological conditions, without additives. In order to achieve a microbicide gel, Chapter 4 presents the synthesis of different conjugates from βCD and the best analogous candidates of BMS806 by [3+2] cycloaddition, which could be tested biologically. Also Chapter 4, we summarize the best conditions for the synthesis of HPG and analogues, a good candidate as a drug support to achieve the desired microbicide. HPG was also conjugated with BMS derivatives through the two reactions studied during this Thesis, the [3+2] cycloaddition and the conjugated addition of thiols to propynamides. Finally, in Chapter 5 all the results obtained in the Laboratory of Molecular Immunobiology at the Gregorio Marañón General University Hospital in Madrid were collected. Cytotoxicity and inhibition of HIV of all samples were analyzed. Some products afford percentages of infection of the cells, after exposure to the virus, which are very promising. Advisors/Committee Members: [email protected] (authoremail), false (authoremailshow), Vilarrasa i Llorens, Jaume (director), Costa i Arnau, Anna M. (director), Vilarrasa i Llorens, Jaume (tutor).

Subjects/Keywords: VIH (Virus); HIV (Viruses); Sida; SIDA; AIDS (Disease); Medicaments antivírics; Antivirales; Antiviral agents; Ciències Experimentals i Matemàtiques; 547

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

APA (6th Edition):

Petit Roig, E. (2019). Bioconjugació de poliols i tiols amb agents antivírics. (Thesis). Universitat de Barcelona. Retrieved from http://hdl.handle.net/10803/667891

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):

Petit Roig, Elena. “Bioconjugació de poliols i tiols amb agents antivírics.” 2019. Thesis, Universitat de Barcelona. Accessed December 08, 2019. http://hdl.handle.net/10803/667891.

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

MLA Handbook (7th Edition):

Petit Roig, Elena. “Bioconjugació de poliols i tiols amb agents antivírics.” 2019. Web. 08 Dec 2019.

Vancouver:

Petit Roig E. Bioconjugació de poliols i tiols amb agents antivírics. [Internet] [Thesis]. Universitat de Barcelona; 2019. [cited 2019 Dec 08]. Available from: http://hdl.handle.net/10803/667891.

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

Council of Science Editors:

Petit Roig E. Bioconjugació de poliols i tiols amb agents antivírics. [Thesis]. Universitat de Barcelona; 2019. Available from: http://hdl.handle.net/10803/667891

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

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