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

  • Bioorg Med Chem. 2007 Feb 15;15(4):1725-31. doi: 10.1016/j.bmc.2006.12.003.
Ravindra K Rawal  1 ,  Rajkamal Tripathi ,  S B Katti ,  Christophe Pannecouque ,  Erik De Clercq
Affiliations
  • 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
PMID: 17178227 DOI: 10.1016/j.bmc.2006.12.003
Abstract

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 microM with minimal toxicity in MT-4 cells as compared to 0.35 microM for thiazobenzimidazole (TBZ). It may be inferred from the present data that majority of compounds in this series exhibit higher selectivity index than TBZ.