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

作者: Maria L. Barreca , Jan Balzarini , Alba Chimirri , Erik De Clercq , Laura De Luca

DOI: 10.1021/JM020977+

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摘要: Starting from 1H,3H-thiazolo[3,4-a]benzimidazoles (TBZs), we performed the design, synthesis, and structure−activity relationship studies of a series 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 RT inhibitors (NNRTIs). Computational were used delineate ligand-RT interactions probe binding ligands RT.

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