2. Academic Validation
  3. Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents

Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents

  • J Med Chem. 2002 Nov 21;45(24):5410-3. doi: 10.1021/jm020977+.
Maria L Barreca 1,  Jan Balzarini,  Alba Chimirri,  Erik De Clercq,  Laura De Luca,  Hans Dieter Höltje,  Monika Höltje,  Anna Maria Monforte,  Pietro Monforte,  Christophe Pannecouque,  Angela Rao,  Maria Zappalà
Affiliations

Affiliation

  • 1 Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy.
PMID: 12431069 DOI: 10.1021/jm020977+
Abstract

Starting from 1H,3H-thiazolo[3,4-a]benzimidazoles (TBZs), we performed the design, synthesis, and the structure-activity relationship studies of a series of 2,3-diaryl-1,3-thiazolidin-4-ones. Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentrations with minimal cytotoxicity, thereby acting as nonnucleoside HIV-1 RT inhibitors (NNRTIs). Computational studies were used to delineate the ligand-RT interactions and to probe the binding of the ligands to HIV-1 RT.

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