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ID: ALA1142217
Journal: Bioorg Med Chem Lett
Title: Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Authors: Côté B, Boulet L, Brideau C, Claveau D, Ethier D, Frenette R, Gagnon M, Giroux A, Guay J, Guiral S, Mancini J, Martins E, Massé F, Méthot N, Riendeau D, Rubin J, Xu D, Yu H, Ducharme Y, Friesen RW.
Abstract: Phenanthrene imidazole 3 (MF63) has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor. This new series was developed by lead optimization of a hit from an internal HTS campaign. Compound 3 is significantly more potent than the previously reported indole carboxylic acid 1 with an A549 whole cell IC(50) of 0.42 microM (50% FBS) and a human whole blood IC(50) of 1.3 microM. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model when orally dosed at 30 and 100mg/kg.
CiteXplore: 18029174