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

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

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):179-83. doi: 10.1016/j.bmcl.2007.10.106.
Mary Mader 1,  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 Jr,  Paul A Lee,  Richard C Schultz,  Jeffrey A Wolos,  Li C Li,  Robert M Campbell,  Bryan D Anderson
Affiliations

Affiliation

  • 1 Eli Lilly and Co., Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA. mader_mary@lilly.com
PMID: 18039577 DOI: 10.1016/j.bmcl.2007.10.106
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.

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