Title: 2-(2,6-Dihalo-phenyl)-3-heteroaryl-2-ylmethyl-1, 3-thiazolidin-4-ones: Anti-HIV agents
Authors: Rawal, Ravindra K ×
Tripathi, Rajkamal
Kulkarni, Smitha
Paranjape, R
Katti, S B
Pannecouque, Christophe
De Clercq, Erik #
Issue Date: Aug-2008
Publisher: Blackwell Munksgaard
Series Title: Chemical Biology & Drug Design vol:72 issue:2 pages:147-154
Abstract: 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 mum as compared to reference parent compound thiazolobenzimidazoles EC(50) 0.35 mum in MT-4 cells.
ISSN: 1747-0277
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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