250264-28-9Relevant articles and documents
Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents - Part VIII
Ferrarini, Pier Luigi,Mori, Claudio,Calderone, Vincenzo,Calzolari, Lorella,Nieri, Paola,Saccomanni, Giuseppe,Martinotti, Enrica
, p. 505 - 513 (1999)
A series of (ethoxycarbonylpiperazinyl)- and piperazinyl- 1,8- naphthyridine derivatives, variously substituted, has been synthesized and pharmacologically investigated for anthihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. On the basis of the pharmacological results, no structure-activity relationship can be deduced at this time. Moreover, the most active compound 4e, was investigated by means of in vitro pharmacological functional studies and in vivo, as a diuretic agent, to determine a possible mechanism of the antihypertensive activity, which results in a probably non-competitive antagonism against α1 vascular adrenoceptors. This mechanism was also shown by the compounds 8 and 13.