Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Bioorg Med Chem Lett
; 20(17): 5080-4, 2010 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-20673717
ABSTRACT
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was identified as a potent P2X(7) antagonist with excellent in vivo activity in animal models of pain, and a profile suitable for progression to clinical studies.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácido Pirrolidonocarboxílico
/
Receptores Purinérgicos P2X7
/
Antagonistas do Receptor Purinérgico P2
/
Amidas
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2010
Tipo de documento:
Article