Biarylimidazoles as inhibitors of microsomal prostaglandin E"2 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.
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