Angiotensin converting enzyme inhibitors: spirapril and related compounds

…, GF Swiss, BR Neustadt, P McNamara…

文献索引：Smith, Elizabeth M.; Swiss, Gerald F.; Neustadt, Bernard R.; McNamara, Paul; Gold, Elijah H.; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 7 p. 1600 - 1606

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被引用次数: 30

摘要

The synthesis of spirapril (5), spiraprilat (25), their RSS stereoisomers, and their glycyl (18b) and lysyl (36, 37) analogues is described. These compounds were evaluated in vivo for inhibition of angiotensin converting enzyme (ACE), and selected compounds were evaluated for in vitro ACE inhibition (spirapril IDM 16 pg/kg; spiraprilat ICm 0.8 nM, ID,,, 8 pg/kg). In anesthetized rats, iv, esters 5 and 36 are more potent than enalapril, and diacids ...