Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
J Med Chem
; 49(25): 7270-3, 2006 Dec 14.
Article
em En
| MEDLINE
| ID: mdl-17149856
ABSTRACT
We describe the discovery and optimization of tertiary carbinamine derived inhibitors of the enzyme beta-secretase (BACE-1). These novel non-transition-state-derived ligands incorporate a single primary amine to interact with the catalytic aspartates of the target enzyme. Optimization of this series provided inhibitors with intrinsic and functional potency comparable to evolved transition state isostere derived inhibitors of BACE-1.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Oxidiazóis
/
Secretases da Proteína Precursora do Amiloide
/
Compostos de Anilina
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2006
Tipo de documento:
Article
País de afiliação:
Estados Unidos