Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1

Microsomal prostaglandin E-2 synthase (mPGES-1) represents a potential target for novel analgesic and anti-inflammatory agents. High-throughput screening identified several leads of mPGES-1 inhibitors which were further optimized for potency and selectivity. A series of inhibitors bearing a biaryl imidazole scaffold exhibits excellent inhibition of PGE(2) production in enzymatic and cell-based assays. The synthesis of these molecules and their activities will be discussed. (C) 2010 Elsevier Ltd. All rights reserved.