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Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives.

Authors
  • Wallace, Owen B
  • Smith, David W
  • Deshpande, Milind S
  • Polson, Craig
  • Felsenstein, Kevin M
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Mar 24, 2003
Volume
13
Issue
6
Pages
1203–1206
Identifiers
PMID: 12643944
Source
Medline
License
Unknown

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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