Synthesis and Biological Evaluation of 2, 3-Diaryl substituted-1, 3-thiazolidin-4-ones as Anti-HIV Agents

Author(s): Ravindra K. Rawal, Raj Kamal Tripathi, S.B. Katti, Christophe Pannecouque, Erik De Clercq.

Journal Name: Medicinal Chemistry

Volume 3 , Issue 4 , 2007

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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 0.204μM concentrations with minimal cytotoxicity to MT-4 cells.

Keywords: Thiazolidin-4-one, metathiazanones, anti-HIV activity, NNRTIs

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Article Details

VOLUME: 3
ISSUE: 4
Year: 2007
Page: [355 - 363]
Pages: 9
DOI: 10.2174/157340607781024393
Price: $58

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