Author/Authors :
Ramani R. Ranatunge، نويسنده , , Richard A. Earl، نويسنده , , David S. Garvey، نويسنده , , David R. Janero، نويسنده , , L. Gordon Letts، نويسنده , , Allison M. Martino، نويسنده , , Madhavi G. Murty، نويسنده , , Stewart K. Richardson، نويسنده , , David J. Schwalb، نويسنده , , Delano V. Young، نويسنده , , Irina S. Zemtseva، نويسنده ,
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 (IC50 for COX-1: >100 μM and COX-2: 1.2 μM).
Keywords :
fax: +1 781 2748080 , e-mail: ramani@nitromed.com , Cyclooxygenase-2 (COX-2) , Pyrazole , Tetrahydrofuran-2-yl.* Corresponding author. Tel.: +1 781 266 4139
