Watthey J W, Stanton J L, Desai M, Babiarz J E, Finn B M
J Med Chem. 1985 Oct;28(10):1511-6. doi: 10.1021/jm00148a023.
Syntheses of the potent angiotensin converting enzyme inhibitor (3S)-1-(carboxymethyl)-3-[[(1S)-1-carboxy-3-phenylpropyl]amino]- 2,3,4,5-tetrahydro-1H-[1]benzazepin-2-one (4b; CGS 14831) and the related monoester prodrug (17a; CGS 14824A) are described together with preparative details for six- and eight-membered ring analogues. Inhibitory potencies and in vivo biological activity of the compounds are discussed. The data indicate that 17a has a biological profile comparable to that of enalapril.
强效血管紧张素转换酶抑制剂(3S)-1-(羧甲基)-3-[[(1S)-1-羧基-3-苯基丙基]氨基]-2,3,4,5-四氢-1H-[1]苯并氮杂卓-2-酮(4b；CGS 14831)及相关单酯前药(17a；CGS 14824A)的合成方法已被描述，同时还介绍了六元环和八元环类似物的制备细节。文中讨论了这些化合物的抑制效力和体内生物活性。数据表明，17a具有与依那普利相当的生物学特性。
