14624-85-2Relevant academic research and scientific papers
Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
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Page 26; 45, (2010/11/30)
A method for the inhibition of the binding of α4β1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either a above, or in formulations for the control or prevention of diseases states in which α4β1 is involved.
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.
