New substituted pyrazole derivatives targeting COXs as potential safe anti-inflammatory agents

Research Abstract

Abstract Background: Everyday studies prove the increasing need for newer and safer agents to control cellular inflammatory response, an underlying cause for the pathophysiology of many other clinical cases. Results: Two newly designed sets of schiff 5a-h and chlacone 6a-f substituted pyrazoles were synthesized and evaluated for their in vivo/ vitro anti-inflammatory activities. Most potent representatives were chosen for investigation of ulcerogenic and molecular docking properties. Conclusion: The synthesized compounds showed considerable edema inhibition percentage range if compared to celecoxib (13-93% and 58-93%, respectively) at different time intervals. Compound 6e showed the best screening results if compared to celecoxib (inhibition %= 93.62% and 93.51% at 5 hours, COX-1/COX-2 selectivity index SI= 215.44 and 308.16 and ulcer index= 7.25 and 8, respectively).

Research Keywords

NSAID; anti-inflammatory; cyclooxygenase; chalcones; schiff; pyrazole; celecoxib; acetophenone; ulcer; docking.