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Bioorg Med Chem. 2009 Jul 1;17(13):4708-17. doi: 10.1016/j.bmc.2009.04.052. Epub 2009 May 3.

Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.

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1
Chemical Sciences, Wyeth Research, Princeton, NJ 08543-8000, USA.

Abstract

gamma-Secretase inhibitors have been shown to reduce the production of beta-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide gamma-secretase inhibitors that reduce beta-amyloid levels in cells is reported. Several examples of compounds within this series demonstrate a higher propensity to inhibit the processing of amyloid precursor protein compared to Notch, an alternative gamma-secretase substrate.

PMID:
19443228
DOI:
10.1016/j.bmc.2009.04.052
[Indexed for MEDLINE]
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