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ID: ALA1143180

Journal: Bioorg Med Chem Lett

Title: Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties.

Authors: Mader M, de Dios A, Shih C, Bonjouklian R, Li T, White W, López de Uralde B, Sánchez-Martinez C, del Prado M, Jaramillo C, de Diego E, Martín Cabrejas LM, Dominguez C, Montero C, Shepherd T, Dally R, Toth JE, Chatterjee A, Pleite S, Blanco-Urgoiti J, Perez L, Barberis M, Lorite MJ, Jambrina E, Nevill CR, Lee PA, Schultz RC, Wolos JA, Li LC, Campbell RM, Anderson BD.

Abstract: Herein we report investigations into the p38alpha 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.

CiteXplore: 18039577

DOI: 10.1016/j.bmcl.2007.10.106