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1: Bioorg Med Chem Lett. 2004 Dec 20;14(24):6049-52.Click here to read Links

3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.

Ranatunge RR, Earl RA, Garvey DS, Janero DR, Letts LG, Martino AM, Murty MG, Richardson SK, Schwalb DJ, Young DV, Zemtseva IS.

NitroMed Inc., 125 Spring St., Lexington, MA 02421, USA. ramani@nitromed.com

A series of 3-(2-methoxytetrahydrofuran-2-yl)pyrazoles (4-10) was synthesized. The compounds were evaluated for their ability to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) activity in human whole blood (HWB). The compound, 5-(4-methanesulfonylphenyl)-3-(2-methoxytetrahydrofuran-2-yl)-1-p-tolyl-1H-pyrazole 5 showed potent and selective COX-2 inhibition (IC50 for COX-1: >100 microM and COX-2: 1.2 microM).

PMID: 15546727 [PubMed - indexed for MEDLINE]