660432-14-4Relevant articles and documents
Synthesis of imidazole based p38 MAP (mitogen-activated protein) kinase inhibitors under buffered conditions
Magnus, Nicholas A.,Diseroad, William D.,Nevill Jr., C. Richard,Wepsiec, James P.
, p. 556 - 560 (2006)
This article describes chemistry that was developed to give access to multigram quantities of imidazole 479754 and several related analogues for Eli Lilly's p38 MAPK program targeting therapies to address inflammation. The molecules of interest have an is
Design of potent and selective 2-aminobenzimidazole-based p38α MAP kinase inhibitors with excellent in vivo efficacy
De Dios, Alfonso,Shih, Chuan,López De Uralde, Beatriz,Sánchez, Concepción,Del Prado, Miriam,Martín Cabrejas, Luisa M.,Pleite, Sehila,Blanco-Urgoiti, Jaime,Lorite, María José,Nevill Jr., C. Richard,Bonjouklian, Rosanne,York, Jeremy,Vieth, Michal,Wang, Yong,Magnus, Nicholas,Campbell, Robert M.,Anderson, Bryan D.,McCann, Denis J.,Giera, Deborah D.,Lee, Paul A.,Schultz, Richard M.,Li, Li C.,Johnson, Lea M.,Wolos, Jeffrey A.
, p. 2270 - 2273 (2007/10/03)
We report the design and discovery of a 2-amino-benzimidazole-based series of potent and highly selective p38α inhibitors. The lead compound 1 had low-nanomolar activity in both ATP competitive enzyme binding and inhibition of TNFα release in macrophages.
