Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives.
Bioorg Med Chem Lett
; 20(3): 1090-3, 2010 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-20034788
ABSTRACT
A series of benzofuran derivatives were prepared to study their antagonistic activities to the A(2A) receptor. Replacement of the ester group of the lead compound 1 with phenyl ring improved the PK profile, while modifications of the amide moiety showed enhanced antagonistic activity. From these studies, compounds 13c, 13f, and 24a showed good potency in vitro and were identified as novel A(2A) receptor antagonists suitable for oral activity evaluation in animal models of catalepsy.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Benzofuranos
/
Receptor A2A de Adenosina
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Antagonistas do Receptor A2 de Adenosina
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article