Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives.
Bioorg Med Chem Lett
; 13(6): 1203-6, 2003 Mar 24.
Article
em En
| MEDLINE
| ID: mdl-12643944
ABSTRACT
Inhibitors of amyloid-beta (Abeta) protein production have been widely pursued as a potential treatment for Alzheimer's disease. Following the identification of a 5 microM screening hit, SAR was initiated using solid-phase synthetic techniques. Two series of alpha-hydroxy esters and ketones which are sub-micromolar inhibitors of Abeta production were identified. The most potent alpha-hydroxyketone identified is approximately 30-fold more potent than the initial lead.
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Base de dados:
MEDLINE
Assunto principal:
Peptídeos beta-Amiloides
/
Ésteres
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article