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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Author(s): M. Ezawa, D. S. Garvey, D. R. Janero, S. P. Khanapure, L. G. Letts, A. Martino, R. R. Ranatunge, D. J. Schwalb and D. V. Young

Volume 2, Issue 1, 2005

Page: [40 - 43] Pages: 4

DOI: 10.2174/1570180053398451

Price: $65

Abstract

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.

Keywords: cyclooxygenase, pyrazole, anti-inflammatory, cox-2, no-cox-2, no-donor


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