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

Abstract

The synthesis of a series of novel 3-(2-methoxytetrahydrofuran-2-yl) pyrazoles and their in vitro cyclooxygenase-2 (COX-2) inhibitory activity in human whole blood (HWB) are reported. 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). © 2004 Elsevier Ltd. All rights reserved.