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

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.