Synthesis and pharmacological activity of angiotensin-converting enzyme inhibitors: N-(mercaptoacyl)-4-substituted-(S)-prolines
| Autor: | Arthur Brown, Rosa Moran, Gerald F. Swiss, Elizabeth M. Smith, Thomas Baum, Peter J.S. Chiu, Edmund J. Sybertz, Elijah H. Gold, Jane A. Sommer, Neustadt Bernard R |
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| Rok vydání: | 1988 |
| Předmět: |
Proline
Bradykinin Angiotensin-Converting Enzyme Inhibitors Peptidyl-Dipeptidase A Structure-Activity Relationship chemistry.chemical_compound In vivo Rats Inbred SHR Drug Discovery medicine Animals Structure–activity relationship Sulfhydryl Compounds Antihypertensive Agents chemistry.chemical_classification biology Angiotensin-converting enzyme Captopril Biological activity Rats Enzyme Biochemistry chemistry Enzyme inhibitor Hypertension biology.protein Molecular Medicine medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 31:875-885 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00399a033 |
| Popis: | The synthesis of a series of N-(mercaptoacyl)-4-substituted-(S)-prolines (2 and 3) is described. These compounds were evaluated in vitro for inhibition of angiotensin-converting enzyme (ACE), and selected compounds were evaluated in vivo for ACE inhibition. The most potent compounds in vitro are 108, 109, 111, 114, and 116, having relative potencies of 1.0, 1.0, 1.3, 1.1, and 2.6 as compared to the potency of captopril. The most potent compounds in vivo intravenously are 108, 111, 114, 116, 117, and 97. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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