The discovery and synthesis of novel adenosine receptor (A(2A)) antagonists.
Bioorg Med Chem Lett
; 15(5): 1333-6, 2005 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-15713381
ABSTRACT
In high throughput screening of our file compounds, a novel structure 1 was identified as a potent A(2A) receptor antagonist with no selectivity over the A1 adenosine receptor. The structure-activity relationship investigation using 1 as a template lead to identification of a novel class of compounds as potent and selective antagonists of A(2A) adenosine receptor. Compound 26 was identified to be the most potent A(2A) receptor antagonist (Ki = 0.8 nM) with 100-fold selectivity over the A1 adenosine receptor.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antagonistas do Receptor A2 de Adenosina
/
Compostos Heterocíclicos com 3 Anéis
/
Antiparkinsonianos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2005
Tipo de documento:
Article
País de afiliação:
Estados Unidos