Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template |
| |
| Authors: | Jane Wang David Limburg Jeff Carter Gabriel Mbalaviele James Gierse Michael Vazquez |
| |
| Institution: | 1. Pfizer Inc. St. Louis Laboratory, PGRD Research, 700 Chesterfield PKWY W, Chesterfield, MO 63017, USA;2. Icagen, Inc. 4222 Emperor Blvd., Suite 350 Durham, NC 27703, USA |
| |
| Abstract: | Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE2 inhibition in a cell-based assay (0.42 μM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF1α. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
