Design, synthesis, and evaluation of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents

Compounds having isothiourea or thiourea functional group have shown high anti-HIV-1 activity. Therefore, a series of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones were designed, synthesized, and evaluated for anti-HIV-1 RT activity. The results of in vitro tests showed that the compound 9 exhibited EC50 at 0.26 μM with minimal toxicity in MT-4 cells as compared to 0.35 μM for thiazobenzimidazole (TBZ). It may be inferred from the present data that majority of compounds in this series exhibit higher selectivity index than TBZ.

In the present study, 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones have been assembled by reflux protocol three component reaction of amine, aldehyde and mercapto acetic acid and tested as HIV-RT inhibitors.Figure optionsDownload as PowerPoint slide