| Literature DB >> 19748780 |
André Giroux1, Louise Boulet, Christine Brideau, Anh Chau, David Claveau, Bernard Côté, Diane Ethier, Richard Frenette, Marc Gagnon, Jocelyne Guay, Sébastien Guiral, Joseph Mancini, Evelyn Martins, Frédéric Massé, Nathalie Méthot, Denis Riendeau, Joel Rubin, Daigen Xu, Hongping Yu, Yves Ducharme, Richard W Friesen.
Abstract
Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imidazole 1 (MF63) with a human whole blood IC50 of 0.20 and 0.14 microM, respectively. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model at oral doses as low as 14 mg/kg. Both active and selective mPGES-1 inhibitors (26 and 44) have a relatively distinct pharmacokinetic profile and are suitable for clinical development.Entities:
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Year: 2009 PMID： 19748780 DOI： 10.1016/j.bmcl.2009.08.085
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823