166895-21-2Relevant 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.
