Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Bioorg Med Chem
; 17(5): 2017-29, 2009 Mar 01.
Article
en En
| MEDLINE
| ID: mdl-19200745
ABSTRACT
Glycogen synthase kinase-3beta (GSK-3beta) is implicated in abnormal hyperphosphorylation of tau protein and its inhibitors are expected to be a promising therapeutic agents for the treatment of Alzheimer's disease. Here we report design, synthesis and structure-activity relationships of a novel series of oxadiazole derivatives as GSK-3beta inhibitors. Among these inhibitors, compound 20x showed highly selective and potent GSK-3beta inhibitory activity in vitro and its binding mode was determined by obtaining the X-ray co-crystal structure of 20x and GSK-3beta.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Oxadiazoles
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Bencimidazoles
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Glucógeno Sintasa Quinasa 3
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Inhibidores Enzimáticos
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Nitrilos
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2009
Tipo del documento:
Article
País de afiliación:
Japón