Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives.
J Med Chem
; 26(9): 1267-77, 1983 Sep.
Article
en En
| MEDLINE
| ID: mdl-6310112
ABSTRACT
The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x),- N-arylalanines (15a,b),-N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic acids (18a-f), and -indoline-2-carboxylic acids (19a-k) is described. In vitro inhibition of angiotensin converting enzyme (ACE) is reported for each compound, and the structure--activity relationship for each series is discussed. The in vivo inhibition of ACE and antihypertensive effects of representative compounds from each series are discussed. The most potent compound, 19d, had an in vitro ACE IC50 of 2.6 X 10(-9) M and lowered blood pressure in spontaneous hypertensive rats 85 mm at a dose of 10 mg/kg po.
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Banco de datos:
MEDLINE
Asunto principal:
Inhibidores de la Enzima Convertidora de Angiotensina
/
Aminoácidos
Límite:
Animals
Idioma:
En
Año:
1983
Tipo del documento:
Article