Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, D. V. Young.

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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Article Details

VOLUME: 2
ISSUE: 1
Year: 2005
Page: [40 - 43]
Pages: 4
DOI: 10.2174/1570180053398451