124953-42-0Relevant articles and documents
New isoxazole derivatives provided with antihypertensive activity
Carenzi,Chiarino,Napoletano,Reggiani,Sala,Sala
, p. 642 - 646 (2007/10/02)
A series of diazacycloalkane-quinazoline derivatives of isoxazoles were synthesized and tested in order to identify new potent and selective α1-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 α1-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 route. Moreover, a higher ratio between oral antihypertensive dosis in SHR and normotensive rats was found with respect to reference compound prazosin.