BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Bioorg Med Chem Lett
; 18(3): 1017-21, 2008 Feb 01.
Article
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| MEDLINE
| ID: mdl-18166458
ABSTRACT
This paper describes the discovery of non-peptidic, potent, and selective hydroxy ethylamine (HEA) inhibitors of BACE-1 by replacement of the prime side of a lead di-amide 2. Inhibitors with nanosmolar potency and high selectivity were identified. Depending on the nature of the P(1)(') and P(2)(') substituents, two different binding modes were observed in X-ray co-crystal structures.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Ácido Aspártico Endopeptidasas
/
Técnicas Químicas Combinatorias
/
Etilaminas
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Secretasas de la Proteína Precursora del Amiloide
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Enfermedad de Alzheimer
Tipo de estudio:
Diagnostic_studies
Límite:
Humans
Idioma:
En
Año:
2008
Tipo del documento:
Article