Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and …

S Klutchko, CJ Blankley, RW Fleming…

文献索引：Klutchko; Blankley; Fleming; Hinkley; Werner; Nordin; Holmes; Hoefle; Cohen; Essenburg Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 1953 - 1961

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被引用次数: 84

摘要

The synthesis and angiotensin converting enzyme (ACE) inhibiting activities of quinapril (CI- 906, 22), its active diacid (CI-928, 33), and its dimethoxy analogue (CI-925, 25) are reported. These tetrahydro-3-isoquinolinecarboxylic acid derivatives possess equivalent in vitro potency and in vivo efficacy to enalapril. Sulfhydryl analogues with the same structural variation are also highly potent. In contrast, tetrahydro-1-isoquinolinecarboxylic acid and ...