Angiotensin converting enzyme inhibitors: spirapril and related compounds

…, GF Swiss, BR Neustadt, P McNamara…

Index: 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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Citation Number: 30

Abstract

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 ...