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

Abstract 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 (IC 50 for COX-1: >100 μM and COX-2: 1.2 μM).