Synthesis, anti-inflammatory, antiplatelet and in silico evaluations of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo3H -benzoxazole-6-yl)-1-phenyl-1H -pyrazole4-yl)acrylamides

Authors : Sultan Baytaş, Nilüfer Nermin Turan Dural, Yeşim Özkan

Pages : 367-382

Doi:10.3906/sag-1302-132

View : 19 | Download : 13

Publication Date : 9999-12-31

Article Type : Makaleler

Abstract :A series of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo-3H-benzoxazole- 6-yl)-1-phenyl-1H-pyrazole-4-yl)acry- lamides (7a--k) were synthesized and evaluated for their in vitro inhibitory activities on COX-1 and COX-2 isoforms using a human whole blood assay as well as their antiplatelet profile against human platelet aggregation using arachidonic acid as agonists. Among the synthesized derivatives 7a--k, especially compound 7g exhibited dual anti-inflammatory and antiplatelet activity with selective COX-2 inhibition.
Keywords : Anti-inflammatory activity, antiplatelet activity, pyrazoles, COX, TXA2 synthetase