- 1-Carboxyalkanoylindoline-2-carboxylic acids
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1-Carboxy-(alkanoyl or aralkanoyl)-indoline-2-carboxylic acids, e.g., those of the formula STR1 R=H, alkyl, alkoxy, halogeno or CF3 ; R'=H or R-phenyl; m=0 or 1; p,q=0 to 2; and derivatives thereof, are antihypertensive and cardioactive agents.
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- Angiotensin Converting Enzyme Inhibitors: 1-Glutarylindoline-2-carboxylic Acid Derivatives
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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*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.
- Gruenfeld, Norbert,Stanton, James L.,Yuan, Andrew M.,Ebetino, Frank H.,Browne, Leslie J.,et al.
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p. 1277 - 1282
(2007/10/02)
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- 1-CARBOXYALKANOYLINDOLINE-2-CARBOXYLIC ACIDS
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1-Carboxy-(alkanoyl or aralkanoyl)-indoline-2-carboxylic acids, e.g., those of the formula STR1 R=H, alkyl, alkoxy, halogeno or CF. sub.3 ; R'=H or R-phenyl;m=0 or 1;p, q=0 to 2; and functional derivatives thereof, are antihypertensive a
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