Substituted Imidazoles as Glucagon Receptor Antagonists
作者： Linda L. Chang , Kelly L. Sidler , Margaret A. Cascieri , Stephen de Laszlo , Greg Koch
DOI: 10.1016/S0960-894X(01)00498-X
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摘要: Abstract A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to identification of a 2- and/or 4-alkyl or alkyloxy substituent on imidazole C4-aryl group as structural determinant significant enhancement in receptor (e.g., 41 , IC 50 =0.053 μM) and selectivity (>1000×) over p38 MAP kinase this class compounds.
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