4.5 Article

Part 2. Notch-sparing γ-secretase inhibitors: The study of novel γ-amino naphthyl alcohols

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 9, Pages 2133-2137

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.03.042

Keywords

Alzheimer's disease; gamma-Secretase inhibitors; gamma-Amino alcohols; Notch-processing; A beta production

Funding

  1. Alzheimer Drug Discovery Foundation
  2. Harvard NeuroDiscovery Center
  3. Center for Neurologic Diseases

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One therapeutic approach for Alzheimer's disease is to inhibit the cleavage of the amyloid precursor protein (APP) by gamma-secretase. At the beginning of a series of studies from our laboratories, a series of novel gamma-amino alcohols (1) were found to possess c-secretase inhibitory activity and Notch-sparing effects. A new one-pot synthesis of gamma-amino alcohols and the structure-activity relationship (SAR) of these analogs will be discussed. (C) 2016 Elsevier Ltd. All rights reserved.

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