ChemInform Abstract: Synthesis and Structure-Activity Relationships of Potent New Angiotensin Converting Enzyme Inhibitors Containing Saturated Bicyclic Amino Acids

Autor:	C. J. Blankley, U. Krolls, H. R. Kaplan, W. M. Pearlman, J. S. Kaltenbronn, D. R. Johnson, Cohen Dm, G. Bobowski, D. E. Dejohn, A. D. Essenburg, A. E. Werner, M. L. Hoefle, L. R. Bennett
Rok vydání:	1987
Předmět:	chemistry.chemical_classification biology Bicyclic molecule Stereochemistry Angiotensin-converting enzyme Captopril General Medicine In vitro Amino acid chemistry In vivo biology.protein medicine Enalapril Proline medicine.drug
Zdroj:	ChemInform. 18
ISSN:	0931-7597
DOI:	10.1002/chin.198747322
Popis:	The synthesis of a series of novel, potent angiotensin converting enzyme (ACE) inhibitors containing saturated bicyclic amino acids in place of proline is described. Octahydroindole-2-carboxylic acid, octahydroisoindole-1-carboxylic acid, and octahydro-3-oxoisoindole-1-carboxylic acid can replace proline in both sulfhydryl and non-sulfhydryl ACE inhibitors to give compounds equipotent to captopril and enalapril both in vitro and in vivo. Structure-activity relationships are discussed. Compound 11a (CI-907, indolapril) has advanced to clinical evaluation.
Databáze:	OpenAIRE
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