864523-75-1Relevant academic research and scientific papers
Benzimidazolone p38 inhibitors
Dombroski, Mark A.,Letavic, Michael A.,McClure, Kim F.,Barberia, John T.,Carty, Thomas J.,Cortina, Santo R.,Csiki, Csilla,Dipesa, Alan J.,Elliott, Nancy C.,Gabel, Christopher A.,Jordan, Crystal K.,Labasi, Jeff M.,Martin, William H.,Peese, Kevin M.,Stock, Ingrid A.,Svensson, Linne,Sweeney, Francis J.,Yu, Chul H.
, p. 919 - 923 (2007/10/03)
The synthesis and in vitro p38α activity of a novel series of benzimidazolone inhibitors is described. The p38α SAR is consistent with a mode of binding wherein the benzimidazolone carbonyl serves as the H-bond acceptor to Met109 of p38α in a manner analogous to the pyridine nitrogen of prototypical pyridylimidazole p38 inhibitors. Potent p38α activity comparable to that of several previously reported p38 inhibitors is observed for this novel chemotype.
