Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties

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• 作者：Mary Mader ; Alfonso de Dios ; Chuan Shih ; Rosanne Bonjouklian ; Tiechao Li ; Wesley White ; Beatriz Ló ; pez de Uralde ; Concepció ; n Sá ; nchez-Martinez ; Miriam del Prado ; Carlos Jaramillo ; Eugenio
• 关键词：p38 MAP kinase ; Inflammation ; Imidazole ; Imidazopyridine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 January 2008
• 年：2008
• 卷：18
• 期：1
• 页码：179-183
• 全文大小：178 K

文摘

Herein we report investigations into the p38α 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.