Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue -, Pages 59-64Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.08.046
Keywords
Cyclooxygenase enzyme; 4-Thiazolidinone; Docking
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Funding
- Turkish Scientific Research Institution (TUBITAK) [111S060]
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In order to develop new selective cyclooxygenase-2 inhibitors, a series of novel 2-aryl-3-(4-sulfamoyl/methylsulfonylphenylamino)-4-thiazolidinones were designed. Molecular modeling studies with COX-2 enzyme were performed by using MOE program. The designed compounds with reasonable binding modes and high docking scores were synthesized. Their COX-1/COX-2 inhibitory activities were evaluated in vitro, using NS-398 and indomethacine as reference compounds. Compounds possessing methyl group (3d and 4d) on the phenyl ring exhibited highly COX-2 inhibitory selectivity and potency. (C) 2012 Elsevier Masson SAS. All rights reserved.
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