Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Bioorg Med Chem Lett
; 20(21): 6231-6, 2010 Nov 01.
Article
en En
| MEDLINE
| ID: mdl-20833041
ABSTRACT
In this Letter, we describe our efforts to design HEA BACE-1 inhibitors that are highly permeable coupled with negligible levels of permeability-glycoprotein activity. These efforts culminate in producing 16 which lowers Αß by 28% and 32% in the cortex and CSF, respectively, in the preclinical wild type Hartley guinea pig animal model when dosed orally at 30mpk BID for 2.5days.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Inhibidores de Proteasas
/
Ácido Aspártico Endopeptidasas
/
Etilaminas
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Secretasas de la Proteína Precursora del Amiloide
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Estados Unidos