Stanton J L, Watthey J W, Desai M N, Finn B M, Babiarz J E, Tomaselli H C
J Med Chem. 1985 Nov;28(11):1603-6. doi: 10.1021/jm00149a010.
The preparation of a series of 3-amino-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-1-acetic acid derivatives 5a-y by reductive amination of 2,3,4,5-tetrahydro-1H-1-benzazepine-2,3-dione (7) with L-amino acid derivatives is described. The compounds were tested for inhibition of angiotensin converting enzyme. The structure-activity profile of the series is discussed. Compound 5a was especially potent when tested in dogs for inhibition of angiotensin I pressor response, having an ID50 = 0.07 mg/kg po.
描述了通过2,3,4,5-四氢-1H-1-苯并氮杂卓-2,3-二酮（7）与L-氨基酸衍生物的还原胺化反应制备一系列3-氨基-2-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓-1-乙酸衍生物5a - y的方法。测试了这些化合物对血管紧张素转换酶的抑制作用。讨论了该系列化合物的构效关系。化合物5a在犬体内测试对血管紧张素I升压反应的抑制作用时表现出特别强的活性，口服半数抑制剂量（ID50）= 0.07 mg/kg。
