|
|||||
|
|
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors |
|
| Authors: | Ranatunge Ramani R Earl Richard A Garvey David S Janero David R Letts L Gordon Martino Allison M Murty Madhavi G Richardson Stewart K Schwalb David J Young Delano V Zemtseva Irina S |
| Affiliation: | NitroMed Inc., 125 Spring St., Lexington, MA 02421, USA |
| 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: | Cyclooxygenase-2 (COX-2) Pyrazole Tetrahydrofuran-2-yl |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |