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

Bioorganic & medicinal chemistry letters 2004 Dec 20; 14(24):6049-52

Link to PubMed abstract

Ranatunge R RR, Earl R RA, Garvey D DS, Janero D DR, Letts L LG, Martino A AM, Murty M MG, Richardson S SK, Schwalb D DJ, Young D DV, Zemtseva I 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).