Il Farmaco 2003-03-01

Anti-HIV agents: design and discovery of new potent RT inhibitors.

Maria Letizia Barreca, Alba Chimirri, Erik De Clercq, Laura De Luca, Anna-Maria Monforte, Pietro Monforte, Angela Rao, Maria Zappalà

Index: Il Farmaco 58 , 259-263, (2003)

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Abstract

This paper reports our work in the field of nonnucleoside RT inhibitors (NNRTIs). On the basis of extensive studies on 1H,3H-thiazolo[3,4-a]benzimidazole derivatives (TBZs) followed by structure-activity relationship (SAR) considerations and molecular modeling, the design and synthesis of a series of 2,3-diaryl-1,3-thiazolidin-4-ones have been performed. Some derivatives proved to be highly effective in inhibiting human immunodeficiency virus type-1 (HIV-1) replication at nanomolar concentrations with minimal toxicity, acting as reverse transcriptase (RT) inhibitors. Computational studies were used in order to probe the binding of our ligands to HIV-1-RT.Copyright 2003 Editions scienctifiques et médicales Elsevier SAS