Dergiler / Turkish Journal of Chemistry / 2012 / Cilt: 36 - Sayı: 3
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
- Sayfa
- 367–382
- DOI
- —
Özet
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.
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.