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

Authors

SULTAN BAYTAŞ
NİLÜFER NERMİN TURAN DURAL
YEŞİM ÖZKAN
HASAN BOLKAN ŞİMŞEK
TÜRKİZ GÜRSEL
SERDAR ÜNLÜ

DOI

10.3906/kim-1110-8

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

First Page

367

Last Page

382

Recommended Citation

BAYTAŞ, SULTAN; DURAL, NİLÜFER NERMİN TURAN; ÖZKAN, YEŞİM; ŞİMŞEK, HASAN BOLKAN; GÜRSEL, TÜRKİZ; and ÜNLÜ, SERDAR (2012) "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: No. 3, Article 2. https://doi.org/10.3906/kim-1110-8
Available at: https://journals.tubitak.gov.tr/chem/vol36/iss3/2