Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors.
Bioorg Med Chem Lett
; 23(13): 3983-7, 2013 Jul 01.
Article
em En
| MEDLINE
| ID: mdl-23683591
ABSTRACT
New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC50=111 nM, EC50=1.78 µM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridonas
/
Triazóis
/
Quinase 3 da Glicogênio Sintase
/
Inibidores de Proteínas Quinases
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article