Diverse combinatorial design, synthesis and inÂ vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors

Article ID	Journal	Published Year	Pages	File Type
7802550	European Journal of Medicinal Chemistry	2012	16 Pages	PDF

Abstract

âº A library of HEPT analogues based on a rational diversity analysis is synthesized. âº The synthesized compounds are evaluated against HIV-1. âº The compounds showed a huge diversity of inhibitory activities against HIV-1. âº Some compounds showed high activity and selectivity index values. âº Diverse combionatorial sub-library design minimizes synthesis and maximizes activity.

Keywords

HEPT N,O-Bis(trimethylsilyl)acetamide TBAI NVP azidothymidine NNRTI EFV AZT 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide BSA Efavirenz MTT PCA Principal component analysis Combinatorial chemistry Combinatorial design Antiviral activity SEM Nevirapine Lawesson’s reagent HIV-1 Human Immunodeficiency Virus type-1 human immunodeficiency virus HIV Tetrabutylammonium iodide

Related Topics

Physical Sciences and Engineering Chemistry Organic Chemistry

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Diverse combinatorial design, synthesis and inÂ vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors

Authors

Raimon Puig-de-la-Bellacasa, Laura Giménez, Sofia Pettersson, Rosalia Pascual, Encarna Gonzalo, José A. Esté, Bonaventura Clotet, José I. Borrell, Jordi Teixidó,