Dual Inhibitors of COX-2 and Soluble Epoxide Hydrolase (sEH)

Abstract

A series of novel Dual Inhibitors of COX-2 and sEH containing an N-urea substituted pyrazole as a lead for sEH inhibition have been synthesized and screened as novel analogues to reduce blood pressure elevation by acting as sEH inhibitors. The synthesized compounds having varying degrees of selectivity towards the sEH enzymes. Particularly compounds 6g and 6i emerged as the most potent sEH inhibitor displaying IC50 values of 0.114 ± 0.014 µM and 0.120 ± 0.03 µM for in-vitro sEH inhibition and the selectivity for COX-2 enzyme pave the way for discovery of novel Dual Inhibitors. Keywords: AUDA, (1, 5)-Diarylpyrazole derivatives, Hypertension, N-Acyl, sEH inhibition, Urea, etc. Read more →