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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3715-20. doi: 10.1016/j.bmcl.2011.04.079. Epub 2011 May 1.

Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.

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  • 1Department of Medicinal Chemistry, Elan Pharmaceuticals, South San Francisco, CA 94080, United States.

Abstract

Herein we describe the structure-activity relationship (SAR) of amino-caprolactam analogs derived from amino-caprolactam benzene sulfonamide 1, highlighting affects on the potency of γ-secretase inhibition, selectivity for the inhibition of APP versus Notch processing by γ-secretase and selected pharmakokinetic properties. Amino-caprolactams that are efficacious in reducing the cortical Aβ(x-40) levels in FVB mice via a single 100 mpk IP dose are highlighted.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21571529
[PubMed - indexed for MEDLINE]
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