Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1 |
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Authors: | Wu Tom Y H Juteau Hélène Ducharme Yves Friesen Richard W Guiral Sébastien Dufresne Lynn Poirier Hugo Salem Myriam Riendeau Denis Mancini Joseph Brideau Christine |
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Affiliation: | Merck Frosst Centre for Therapeutic Research, Kirkland, Quebec, Canada. |
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Abstract: | 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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