Anti-HIV agents: design and discovery of new potent RT inhibitors
Barreca, Maria Letizia × Chimirri, Alba De Clercq, Erik De Luca, Laura Monforte, Anna-Maria Monforte, Pietro Rao, Angela Zappalà, Maria #
Farmaco (Società chimica italiana : 1989) vol:58 issue:3 pages:259-63
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.