Title: Synthesis and Biological Evaluation of 2, 3-Diaryl substituted-1, 3-thiazolidin-4-ones as Anti-HIV Agents
Volume: 3
Issue: 4
Author(s): Ravindra K. Rawal, Raj Kamal Tripathi, S.B. Katti, Christophe Pannecouque and Erik De Clercq
Affiliation:
Keywords:
Thiazolidin-4-one, metathiazanones, anti-HIV activity, NNRTIs
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.
