Design of a Heteroaryl Modified, 1,5-Disubstituted Pyrazole Cyclooxygenase-2 (COX-2) Selective Inhibitor

M. Ezawa, D. Garvey, D. Janero, S. Khanapure, L. Letts, A. Martino, R. Ranatunge, D. Schwalb, D. Young
2005 Letters in Drug Design & Discovery  
Vicinal 1-(4-methylsulfonyl)benzene-5-(3-pyridyl) substituted pyrazole compound containing a nitric oxide (NO)-donating group at the 3-position of the pyrazole ring was synthesized and evaluated for its ability to inhibit COX isozymes in human whole blood. We report here the synthesis of 4-{3-[(1Z)-4-(nitrooxy)but-1-enyl]-5-(3-pyridyl)pyrazolyl}-1-(4-methylsulfonyl)benzene (9) and its COX-2 inhibitory potency.
doi:10.2174/1570180053398451 fatcat:irj3tye7jjgbxbao6sdba2rdlu