کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376058 | 981949 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
Phenanthrene imidazole 3 has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 24, 15 December 2007, Pages 6816–6820
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 24, 15 December 2007, Pages 6816–6820
نویسندگان
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,