Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett
; 22(24): 7555-61, 2012 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-23140885
ABSTRACT
A series of thiazole derivatives were designed, and prepared to develop RAGE antagonist for the treatment of Alzheimer's disease (AD). SAR studies were performed to optimize inhibitory activity on Aß-RAGE binding. SAR studies showed that introducing an amino group at part A was essential for inhibitory activity on Aß-RAGE binding. Compounds selected from Aß-RAGE binding screening displayed inhibitory activity on Aß transport across BBB. They also showed inhibitory activity against Aß-induced NF-κB activation. These results indicated that our derivatives had a potential as therapeutic agent for the treatment of AD.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
/
Receptores Imunológicos
/
Doença de Alzheimer
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2012
Tipo de documento:
Article