Angiotensin converting enzyme inhibitors: 1-glutarylindoline-2-carboxylic acids derivatives.

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Gruenfeld N, Stanton JL, Yuan AM, Ebetino FH, Browne LJ, Gude C, Huebner CF

Angiotensin converting enzyme inhibitors: 1-glutarylindoline-2-carboxylic acids derivatives.

J Med Chem. 1983 Sep;26(9):1277-82.

PubMed ID

6310113 [ View in PubMed

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Abstract

The preparation of a series of 1-glutarylindoline-2(S)-carboxylic acid derivatives, 6a-v and 21a-c, is described. The above compounds were tested for inhibition of angiotensin converting enzyme. The structure-activity relationship of the series is also discussed. Compound 6u, the most potent member of the series, had an in vitro IC50 of 4.8 X 10(-9) M. Compound 6v, an ethyl ester of 6u, lowered blood pressure 70 mm in spontaneous hypertensive rats at an oral dose of 30 mg/kg.

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