Anti-HIV agents: design and discovery of new potent RT inhibitors.
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.
Barreca
Maria Letizia
ML
Dipartimento Farmaco-Chimico, Università degli Studi di Messina, Viale Annunziata, 98168 Messina, Italy.
Chimirri
Alba
A
De Clercq
Erik
E
De Luca
Laura
L
Monforte
Anna-Maria
AM
Monforte
Pietro
P
Rao
Angela
A
Zappalà
Maria
M
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D015195:Drug Design; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology*; D006801:Humans; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013678:Technology, Pharmaceutical / Q000379:methods
D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors