Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo

S Thaisrivongs, DT Pals, DW Harris…

文献索引：Thaisrivongs, Suvit; Pals, Donald T.; Harris, Douglas W.; Kati, Warren M.; Turner, Steve R. Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 2088 - 2093

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被引用次数: 65

摘要

A structure-activity analysis of peptides containing backbone C"-methyl and No-methyl modifications led to the discovery of potent renin inhibitors with high metabolic stability. In vitro, Boc-Pro-Phe-N"-MeHis-Leu $-[CHOHCH,] Val-Ile-Amp (XII) is a potent inhibitor of human plasma renin with ICso of 0.26 nM. It is a much weaker inhibitor of other aspartic proteases such as porcine pepsin or bovine cathepsin D (ICso= 6 KM). It was shown not to ...