Authors: SULTAN BAYTAŞ, NİLÜFER NERMİN TURAN DURAL, YEŞİM ÖZKAN, HASAN BOLKAN ŞİMŞEK, TÜRKİZ GÜRSEL, SERDAR ÜNLÜ
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, TXA_2 synthetase
Full Text: PDF