Title: Synthesis and biological evaluation of 2,3-diaryl substituted-1,3-thiazolidin-4-ones as anti-HIV agents
Authors: Rawal, Ravindra K ×
Tripathi, Raj Kamal
Katti, S B
Pannecouque, Christophe
De Clercq, Erik #
Issue Date: Jul-2007
Series Title: Medicinal chemistry (Sh⁻ariqah, United Arab Emirates) vol:3 issue:4 pages:355-63
Abstract: A series of 1,3-thiazolidin-4-ones and metathiazanones were synthesized and evaluated as anti-HIV agents. The results of the in vitro assays showed that some of the synthesized compounds were effective inhibitor of reverse transcriptase enzyme of human immunodeficiency virus type-1 (HIV-1) at micromolar concentrations with less cytotoxicity in MT-4 cells as compared to thiazolobenzimidazole (TBZ). Structure-activity relationship studies revealed that the nature of the substituents at the 2 and 3 positions of the thiazolidin-4-one nucleus had a significant impact on the in vitro anti-HIV activity of this class of antiretroviral agents. One of the compounds, 1, inhibited the enzyme at 0.204 microM concentrations with minimal cytotoxicity to MT-4 cells.
ISSN: 1573-4064
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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