Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376058 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
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 IC50 of 0.42 μM (50% FBS) and a human whole blood IC50 of 1.3 μM. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model when orally dosed at 30 and 100 mg/kg.
Graphical abstractPhenanthrene imidazole 3 has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Bernard Côté, Louise Boulet, Christine Brideau, David Claveau, Diane Ethier, Richard Frenette, Marc Gagnon, André Giroux, Jocelyne Guay, Sébastien Guiral, Joseph Mancini, Evelyn Martins, Frédéric Massé, Nathalie Méthot, Denis Riendeau, Joel Rubin,