Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists

…, WR Schoen, ML MacDougall, JN Livingston

文献索引：Ladouceur, Gaetan H.; Cook, James H.; Doherty, Elizabeth M.; Schoen, William R.; MacDougall, Margit L.; Livingston, James N. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 3 p. 461 - 464

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被引用次数: 37

摘要

5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure–activity relationships led to the discovery of a potent antagonist, IC50= 0.11 μM, more than 60-fold improvement over the lead structure.