Premium
2‐(2,6‐Dihalo‐phenyl)‐3‐heteroaryl‐2‐ylmethyl‐1, 3‐thiazolidin‐4‐ones: Anti‐HIV agents
Author(s) -
Rawal Ravindra K.,
Tripathi Rajkamal,
Kulkarni Smitha,
Paranjape R.,
Katti S. B.,
Pannecouque Christophe,
De Clercq Erik
Publication year - 2008
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2008.00683.x
Subject(s) - reverse transcriptase , chemistry , in vitro , cytotoxicity , aryl , enzyme , amine gas treating , human immunodeficiency virus (hiv) , stereochemistry , ic50 , biochemistry , virology , biology , organic chemistry , rna , gene , alkyl
A diversity of novel 2‐aryl‐3‐heteroaryl‐2‐ylmethyl‐1,3‐thiazolidin‐4‐ones were designed and synthesized by reacting heteroaryl‐2‐ylmethyl amine with various 2,6‐dihalosubstituted benzaldehydes and mercaptoacetic acid. The title compounds were evaluated for human immunodeficiency virus type‐1 (HIV‐1) reverse transcriptase (RT) inhibitory activity. The results of in vitro assays showed that some of the compounds were effective inhibitors of HIV‐1 reverse transcriptase enzyme at micromolar concentrations with less cytotoxicity in both MT‐4 cells as well as acutely infected human T‐lymphoid CEM cells. Compounds 4h and 4k emerged as moderately more potent with EC 50 are at 0.20 and 0.21 μ m as compared to reference parent compound thiazolobenzimidazoles EC 50 0.35 μ m in MT‐4 cells.