Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists.
Bioorg Med Chem Lett
; 18(16): 4477-81, 2008 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-18674903
ABSTRACT
Replacement of the core beta-amino acid in our previously reported piperidine acetic acid and beta-phenylalanine-based Bradykinin B1 antagonists by dihydroquinoxalinone acetic acid increases the in vitro potency and metabolic stability. The most potent compounds from this series have IC(50)s<0.2 nM in a human B1 receptor functional assay. A molecular modeling study of the binding modes of key compounds, based on a B1 homology model, explains the structure-activity relationship (SAR) for these analogs.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Quinoxalinas
/
Química Farmacêutica
/
Receptor B1 da Bradicinina
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Antagonistas de Receptor B1 da Bradicinina
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Acetamidas
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article