Synthesis and Na+/H+ exchanger inhibitory activity of benzoylguanidine derivatives.
Eur J Med Chem
; 46(9): 4107-16, 2011 Sep.
Article
en En
| MEDLINE
| ID: mdl-21724305
ABSTRACT
Twenty-two compounds of substituted benzoylguanidine derivatives were designed and synthesized as potent NHE1 inhibitors. Twelve compounds showed more potent NHE1 inhibitory activity than cariporide. The activities of compounds 7e, 7h and 7j (IC(50) = 0.073 ± 0.021, 0.084 ± 0.012 and 0.068 ± 0.021 nmol/L, respectively) were two orders of magnitude higher than that of cariporide (30.7 ± 2.5 nmol/L). Myocardial cells in vitro screening showed 7j had highlighted protective effect on cardiomyocytes subjected to hypoxia/reoxygenation. Thus it is valuable for further investigation.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Intercambiadores de Sodio-Hidrógeno
/
Guanidinas
Límite:
Animals
Idioma:
En
Revista:
Eur J Med Chem
Año:
2011
Tipo del documento:
Article
País de afiliación:
China
Pais de publicación:
FR
/
FRANCE
/
FRANCIA
/
FRANÇA