234766-95-1Relevant academic research and scientific papers
Substituted imidazoles as glucagon receptor antagonists
Chang, Linda L.,Sidler, Kelly L.,Cascieri, Margaret A.,De Laszlo, Stephen,Koch, Greg,Li, Bing,MacCoss, Malcolm,Mantlo, Nathan,O'Keefe, Stephen,Pang, Margaret,Rolando, Anna,Hagmann, William K.
, p. 2549 - 2553 (2007/10/03)
A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC50 = 0.053 μM) and selectivity (> 1000 ×) over p38 MAP kinase in this class of compounds.
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase
Liverton, Nigel J.,Butcher, John W.,Claiborne, Christopher F.,Claremon, David A.,Libby, Brian E.,Nguyen, Kevin T.,Pitzenberger, Steven M.,Selnick, Harold G.,Smith, Garry R.,Tebben, Andrew,Vacca, Joseph P.,Varga, Sandor L.,Agarwal, Lily,Dancheck, Kim,Forsyth, Amy J.,Fletcher, Daniel S.,Frantz, Betsy,Hanlon, William A.,Harper, Coral F.,Hofsess, Scott J.,Kostura, Matthew,Lin, Jiunn,Luell, Sylvie,O'Neill, Edward A.,Orevillo, Chad J.,Pang, Margaret,Parsons, Janey,Rolando, Anna,Sahly, Yousif,Visco, Denise M.,O'Keefe, Stephen J.
, p. 2180 - 2190 (2007/10/03)
Novel potent and selective diarylimidazole inhibitors of p38 MAP (mitogen-activated protein) kinase are described which have activity in both cell-based assays of tumor necrosis factor-α (TNF-α) release and an animal model of rheumatoid arthritis. The SAR
