Synthesis of Chalcone Derivatives as COX-2 Inhibitory Activity for Ischemic Stroke Treatment.

Cyclooxygenase (COX)-2 is a crucial mediator contributing to blood–brain barrier damage during cerebral ischemia. The ability of target compounds to inhibit COX-1 and COX-2 enzymes was determined. Compound 4a showed a high COX-2 inhibitory potency and selectivity, which was higher activity than observed for the positive control celecoxib. A docking study was performed for compound 4a to explain its interaction with the COX-2 receptor active site. [ABSTRACT FROM AUTHOR]