Title of article
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors
Author/Authors
Bernard Côté، نويسنده , , Louise Boulet، نويسنده , , Christine Brideau، نويسنده , , David Claveau، نويسنده , , Diane Ethier، نويسنده , , Richard Frenette، نويسنده , , Marc Gagnon، نويسنده , , André Giroux، نويسنده , , Jocelyne Guay، نويسنده , , Sébastien Guiral، نويسنده , , Joseph Mancini، نويسنده , , Evelyn Martins، نويسنده , , Frédéric Massé، نويسنده , , Nathalie Méthot، نويسنده , , Denis Riendeau، نويسنده , , Joel Rubin، نويسنده , , Daigen Xu، نويسنده , , Hongping Yu، نويسنده , , Yves Ducharme، نويسنده , , Richard W. Friesen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
6816
To page
6820
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.
Keywords
Prostanoid , mPGES-1 , inflammation , PGE2
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798892
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