Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties
作者:Mary Mader、Alfonso de Dios、Chuan Shih、Rosanne Bonjouklian、Tiechao Li、Wesley White、Beatriz López de Uralde、Concepción Sánchez-Martinez、Miriam del Prado、Carlos Jaramillo、Eugenio de Diego、Luisa M. Martín Cabrejas、Carmen Dominguez、Carlos Montero、Timothy Shepherd、Robert Dally、John E. Toth、Arindam Chatterjee、Sehila Pleite、Jaime Blanco-Urgoiti、Leticia Perez、Mario Barberis、María José Lorite、Enrique Jambrina、C. Richard Nevill、Paul A. Lee、Richard C. Schultz、Jeffrey A. Wolos、Li C. Li、Robert M. Campbell、Bryan D. Anderson
DOI:10.1016/j.bmcl.2007.10.106
日期:2008.1
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.