Angiotensin converting enzyme inhibitors: structure-activity profile of 1-benzazepin-2-one derivatives.

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Stanton JL, Watthey JW, Desai MN, Finn BM, Babiarz JE, Tomaselli HC

Angiotensin converting enzyme inhibitors: structure-activity profile of 1-benzazepin-2-one derivatives.

J Med Chem. 1985 Nov;28(11):1603-6.

PubMed ID

2999394 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Captopril	Angiotensin-converting enzyme	IC 50 (nM)	15	N/A	N/A	Details
Enalapril	Angiotensin-converting enzyme	IC 50 (nM)	4.5	N/A	N/A	Details