SYNTHESIS, BIOLOGICAL EVALUATION OF 3-CHLORO-4-(4-METHANESULFONYL-PHENYL)-1-PHENYL-AZETIDIN-2-ONE AND 5-(4-METHANESULFONYL-PHENYL)-3-PHENYL-THIAZOLIDIN-4-ONE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS
Abstract
A series of 3-Chloro-4-(4-Methanesulfonyl-phenyl)-1-phenyl-azetidin-2-one and 5-(4-Methanesulfonyl-phenyl)-3-phenyl-thiazolidin-4-one derivatives were synthesized with a pharmacophoric group of 4-methanesulfonyl group at the para position of one of the aryl rings and characterized by IR,NMR, mass spectral and elemental analyses. All the synthesized compounds were tested at a concentration of 20μM against COX-1 and COX-2 enzymes by Colorimetric COX Inhibitor Screening Assay. From both the derivatives, compd-5, compd- 7 and compd- 10 were found to be active selectively exhibited 65.5%, 72.5% and 66.9% respectively, against COX-2 enzyme.
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