Benzolactams. A new class of converting enzyme inhibitors
| Autor: | B.I. Lamont, J. L. Davidson, David Taub, Eugene D. Thorsett, William H. Parsons, Aster Sd, Arthur A. Patchett, E. H. Ulm |
|---|---|
| Rok vydání: | 1983 |
| Předmět: |
chemistry.chemical_classification
Steric effects Lactams Stereochemistry Biophysics Molecular Conformation Angiotensin-Converting Enzyme Inhibitors Cell Biology Biochemistry chemistry.chemical_compound Structure-Activity Relationship Enzyme chemistry Side chain Lactam Indicators and Reagents Molecular Biology |
| Zdroj: | Biochemical and biophysical research communications. 117(1) |
| ISSN: | 0006-291X |
| Popis: | A series of potent inhibitors of angiotensin-converting enzyme (dipeptidyl carboxy-peptidase, E.C. 3.4.15.1) derived from benzofused 1-carboxyalkyl-3-(1-carboxy-3-phenylpropylamino) lactams ( III ) is described. In the most effective inhibitors (I50 2-4X10−9M) the lactam is 7 or 8 membered and the N-1 side chain is carboxymethyl or carboxyethyl. Conformational and steric factors pertinent to binding to the enzyme are discussed. |
| Databáze: | OpenAIRE |
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