Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1

Microsomal prostaglandin E2 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 PGE2 production in enzymatic and cell-based assays. The synthesis of these molecules and their activities will be discussed.

Graphical abstractBiarylimidazoles were prepared and evaluated as inhibitors of microsomal prostaglandin E2 synthase-1.Figure optionsDownload full-size imageDownload as PowerPoint slide