Dicarboxylic acid dipeptide neutral endopeptidase inhibitors

…, RD Ghai, R deJesus, C Diefenbacher…

文献索引：Ksander, Gary M.; Ghai, Raj D.; deJesus, Reynalda; Diefenbacher, Clive G.; Yuan, Andrew; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 10 p. 1689 - 1700

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被引用次数: 39

摘要

The synthesis of three series of dicarboxylic acid dipeptide neutral endopeptidase 24.11 (NEP) inhibitors is described. In particular, the amino butyramide 21a exhibited potent NEP inhibitory activity (IC50= 5.0 nM) in vitro and in vivo. Blood levels of 21s were determined using an ex vivo method by measuring plasma inhibitory activity in conscious rats, mongrel dogs, and cynomolgus monkeys. Free drug concentrations were 10-1500 times greater ...