Biarylimidazoles as inhibitors of microsomal prostaglandin E 2 synthase-1

…, Y Ducharme, RW Friesen, S Guiral, L Dufresne…

Index: Wu, Tom Y.H.; Juteau, Helne; Ducharme, Yves; Friesen, Richard W.; Guiral, Sebastien; Dufresne, Lynn; Poirier, Hugo; Salem, Myriam; Riendeau, Denis; Mancini, Joseph; Brideau, Christine Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 23 p. 6978 - 6982

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Citation Number: 22

Abstract

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 ...