Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.
Bioorg Med Chem Lett
; 17(10): 2921-6, 2007 May 15.
Article
em En
| MEDLINE
| ID: mdl-17412584
ABSTRACT
A series of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety were synthesized and evaluated as a novel class of AT(1) receptor antagonists. Among them, compounds 10a and 10g inhibited [(125)I] AngII-binding affinity to AT(1) receptor at nanomolar level and potently inhibited the Ang II-induced pressor response by oral administration. Moreover, evaluation in spontaneously hypertensive rats showed that 10a is an orally active AT(1) receptor antagonist.
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Base de dados:
MEDLINE
Assunto principal:
Bloqueadores do Receptor Tipo 1 de Angiotensina II
Limite:
Animals
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article