A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity

…, BD Stevens, MT Didiuk, M Tu, C Perreault…

文献索引：Filipski, Kevin J.; Bian, Jianwei; Ebner, David C.; Lee, Esther C.Y.; Li, Jian-Cheng; Sammons, Matthew F.; Wright, Stephen W.; Stevens, Benjamin D.; Didiuk, Mary T.; Tu, Meihua; Perreault, Christian; Brown, Janice; Atkinson, Karen; Tan, Beijing; Salatto, Christopher T.; Litchfield, John; Pfefferkorn, Jeffrey A.; Guzman-Perez, Angel Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 415 - 420

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被引用次数: 12

摘要

A novel series of glucagon receptor antagonists has been discovered. These pyrazole ethers and aminopyrazoles have lower molecular weight and increased polarity such that the molecules fall into better drug-like property space. This work has culminated in compounds 44 and 50 that were shown to have good pharmacokinetic attributes in dog, in contrast to rats, in which clearance was high; and compound 49, which demonstrated a ...