Synthesis and evaluation of antihypertensive activity of 1,8-naphthyridine derivatives. Part X.
Eur J Med Chem
; 36(11-12): 925-34, 2001.
Article
em En
| MEDLINE
| ID: mdl-11755235
ABSTRACT
A series of 4-(N-methylencycloalkylamino)-1,8-naphthyridine derivatives variously substituted in positions 2 and 7 were synthesized and pharmacologically investigated for possible antihypertensive activity. These compounds were tested to determine a possible vasodilator mechanism of action. Compounds 22, 23, 27-29, 47 and 48 showed satisfactory levels of potency (pIC(50)>5), which in one case (compound 23) reached a really interesting value (pIC(50) 6.92). Furthermore, for some selected compounds (19, 22, 23, 26, 28, 29, 47), the vasorelaxing activity was also evaluated in the presence of the guanylate cyclase blocker ODQ or of the adenylate cyclase blocker SQ 22536, and some of these can be considered as possible guanylate-cyclase inhibitors. Finally, compounds 19, 22 and 23 were also tested in the presence of the ATP-sensitive potassium channel blocker glybenclamide and seem to possess activating properties on these potassium channels.
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Vasodilatação
/
Naftiridinas
/
Anti-Hipertensivos
Limite:
Animals
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article