Title of article :
Synthesis, anti-inflammatory, antiplatelet and in silico evaluations of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo- 3H-benzoxazole-6-yl)-1-phenyl-1H-pyrazole- 4-yl)acrylamides
Author/Authors :
BAYTAS, Sultan Gazi Üniversitesi - Faculty of Pharmacy - Department of Pharmaceutical Chemistry, TURKEY , TURAN DURAL, Nil¨ufer Nermin Gazi Üniversitesi - Faculty of Pharmacy - Department of Pharmacology, TURKEY , OZKAN, Ye¸sim Gazi Üniversitesi - Faculty of Pharmacy - Department of Biochemistry, TURKEY , S¸IMS¸EK, Hasan Bolkan Gazi Üniversitesi - Faculty of Pharmacy - Department of Biochemistry, TURKEY , G¨URSEL, T¨urkiz Gazi Üniversitesi - School of Medicine - Department of Pediatrics, TURKEY , UNLU, Serdar Gazi Üniversitesi - Faculty of Pharmacy - Department of Pharmaceutical Chemistry, TURKEY
Abstract :
A series of (E) -3-(3-(2,3-dihydro-3-methyl-2-oxo-3H -benzoxazole-6-yl)-1-phenyl-1H -pyrazole-4-yl) acrylamides (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
Journal title :
Turkish Journal of Chemistry
Journal title :
Turkish Journal of Chemistry
