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

[ Vol. 3 , Issue. 4 ]

Author(s):

Ravindra K. Rawal, Raj Kamal Tripathi, S.B. Katti, Christophe Pannecouque and Erik De Clercq   Pages 355 - 363 ( 9 )

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

Affiliation:

Medicinal&Process Chemistry Division, bMicrobiology Division, Central Drug Research Institute,Lucknow-226 001, India.



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