4.5 Article

Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38 alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 1, 页码 179-183

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.10.106

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p38 MAP kinase; inflammation; imidazole; imidazopyridine

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Herein we report investigations into the p38 alpha MAP kinase activity of trisubstituted imidazoles that led to the identification of compounds possessing highly potent in vivo activity. The SAR of a novel series of imidazopyridines is demonstrated as well, resulting in compounds possessing cellular potency and enhanced in vivo activity in the rat collagen-induced arthritis model of chronic inflammation. (C) 2007 Elsevier Ltd. All rights reserved.

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