Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.
Bioorg Med Chem Lett
; 20(16): 4951-4, 2010 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-20634071
ABSTRACT
A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity relationships (SAR) were investigated both with respect to activity at the P2X(7) receptor and in vitro metabolic stability. Compound 10 was identified as a potent P2X(7) antagonist with reduced in vitro metabolism and high solubility.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Anti-Inflamatórios não Esteroides
/
Antagonistas do Receptor Purinérgico P2
/
Imidazóis
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article