Angiotensin converting enzyme inhibitors: 1-glutarylindoline-2-carboxylic acid derivatives
| Autor: | Frank H. Ebetino, Norbert Gruenfeld, Leslie J. Browne, Candido Gude, Charles F. Huebner, Andrew M. Yuan, James L. Stanton |
|---|---|
| Rok vydání: | 1983 |
| Předmět: |
Oral dose
Binding Sites Indoles Magnetic Resonance Spectroscopy biology chemistry.chemical_element Angiotensin-Converting Enzyme Inhibitors Blood Pressure Rats Inbred Strains Angiotensin-converting enzyme Zinc Nuclear magnetic resonance spectroscopy Ethyl ester Medicinal chemistry In vitro Rats chemistry Drug Discovery biology.protein Animals Molecular Medicine Binding site IC50 |
| Zdroj: | Journal of Medicinal Chemistry. 26:1277-1282 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00363a012 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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