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.
NAPHTHYRIDININONES AS AURORA KINASE INHIBITORS
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Page/Page column 57-58, (2010/04/03)
Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative di