The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.
Bioorg Med Chem Lett
; 23(2): 466-71, 2013 Jan 15.
Article
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| MEDLINE
| ID: mdl-23253441
ABSTRACT
In an attempt to further improve overall profiles of the oxadiazine series of GSMs, in particular the hERG activity, conformational modifications of the core structure resulted in the identification of fused oxadiazepines such as 7i which had an improved hERG inhibition profile and was a highly efficacious GSM in vitro and in vivo in rats. These SAR explorations offer opportunities to identify potential drugs to treat Alzheimer's disease.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Azepinas
/
Canales de Potasio Éter-A-Go-Go
/
Secretasas de la Proteína Precursora del Amiloide
/
Descubrimiento de Drogas
/
Enfermedad de Alzheimer
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article
País de afiliación:
Estados Unidos