Angiotensin converting enzyme inhibitors: 1-glutarylindoline-2-carboxylic acid derivatives

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Abstract
The preparation of a series of 1-glutarylindoline-2(S)-carboxylic acid derivatives is described. The compounds were tested for inhibition of angiotensin converting enzyme. The structure-activity relationship of the series is also discussed. 1-[(2R,4R)-4-Carboxy-2-methyl-4-(2-phenylethyl)-butyryl]indoline-2(S)-carboxylic acid, the most potent member of the series, had an in vitro IC50 [median inhibitory concentration] of 4.8 .times. 10-9 M. The ethyl ester of this compound, lowered blood pressure 70 mm in spontaneous hypertensive rats at an oral dose of 30 mg/kg.