Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists

P Madsen, LB Knudsen, FC Wiberg…

文献索引：Madsen, Peter; Knudsen, Lotte B.; Wiberg, Finn C.; Carr, Richard D. Journal of Medicinal Chemistry, 1998 , vol. 41, # 26 p. 5150 - 5157

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被引用次数: 94

摘要

The first non-peptide competitive human glucagon receptor antagonist, 2-(benzimidazol-2- ylthio)-1-(3, 4-dihydroxyphenyl)-1-ethanone, NNC 92-1687 (2), is described. This antagonist has a binding affinity of 20 μM (IC50) and a functional K i= 9.1 μM at the human glucagon receptor. A structure-activity relationship (SAR) was obtained on this compound, and the results show that only the benzimidazole part can be changed without complete loss of ...