Title: Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents
Authors: Barreca, Maria L ×
Balzarini, Jan
Chimirri, Alba
De Clercq, Erik
De Luca, Laura
Höltje, Hans Dieter
Höltje, Monika
Monforte, Anna Maria
Monforte, Pietro
Pannecouque, Christophe
Rao, Angela
Zappalà, Maria #
Issue Date: Nov-2002
Series Title: Journal of Medicinal Chemistry vol:45 issue:24 pages:5410-3
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.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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