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

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

doi:10.2174/1570180053398451

ISSN: 1570-1808
E-ISSN: 1875-628X

Design of a Heteroaryl Modified, 1,5-Disubstituted Pyrazole Cyclooxygenase-2 (COX-2) Selective Inhibitor
Authors: M. Ezawa¹, D. S. Garvey², D. R. Janero³, S. P. Khanapure⁴, L. G. Letts⁵, A. Martino⁶, R. R. Ranatunge⁷, D. J. Schwalb⁸ and D. V. Young⁹
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¹ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ² NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ³ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ⁴ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ⁵ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ⁶ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ⁷ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ⁸ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA. ⁹ NitroMed, Inc., 125 Spring Street, Lexington, MA 02421, USA.
Source: Letters in Drug Design & Discovery, Volume 2, Issue 1, Feb 2005, p. 40 - 43
DOI: https://doi.org/10.2174/1570180053398451
- Available online: 01 Feb 2005

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.

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2005-02-01

2025-05-28

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Article Type: Review Article

Keyword(s): anti-inflammatory; cox-2; cyclooxygenase; no-cox-2; no-donor; pyrazole

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

Abstract

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