New isoxazole derivatives provided with antihypertensive activity.
Arzneimittelforschung
; 39(6): 642-6, 1989 Jun.
Article
en En
| MEDLINE
| ID: mdl-2775328
ABSTRACT
A series of diazacycloalkane-quinazoline derivatives of isoxazoles were synthesized and tested in order to identify new potent and selective alpha 1-antagonists. A preliminary screening by using in vitro tests such as binding assay (3H-prazosin and 3H-rauwolscine displacement) and analysis of antagonistic activity in isolated rat aorta (norepinephrine-induced response) and in isolated rat vas deferens (clonidine-induced response) indicated that many of these compounds exhibited a good affinity and selectivity towards alpha 1-adrenergic receptors associated with potent pharmacological activity. In particular, a 3-bromo-5-isoxazolecarbonyl derivative, selected for further in vivo investigation, was provided with as high antihypertensive action as prazosin in spontaneously hypertensive rats (SHR) coupled to a shallow dose-response curve by oral route. Moreover, a higher ratio between oral antihypertensive doses in SHR and normotensive rats was found with respect to reference compound prazosin.
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Banco de datos:
MEDLINE
Asunto principal:
Oxazoles
/
Isoxazoles
/
Antihipertensivos
Límite:
Animals
Idioma:
En
Año:
1989
Tipo del documento:
Article