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.
Anti-inflammatory activity, antiplatelet activity, pyrazoles, COX, TXA_2 synthetase
BAYTAŞ, SULTAN; DURAL, NİLÜFER NERMİN TURAN; ÖZKAN, YEŞİM; ŞİMŞEK, HASAN BOLKAN; GÜRSEL, TÜRKİZ; and ÜNLÜ, SERDAR
"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,"
Turkish Journal of Chemistry: Vol. 36:
3, Article 2.
Available at: https://journals.tubitak.gov.tr/chem/vol36/iss3/2