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Bioorg Med Chem Lett. 2016 May 1;26(9):2133-7. doi: 10.1016/j.bmcl.2016.03.042. Epub 2016 Mar 15.

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

Author information

1
Laboratory for Experimental Alzheimer Drugs (LEAD), Center for Neurologic Diseases, Harvard Medical School and Brigham and Women's Hospital, 77 Avenue Louis Pasteur, Harvard Institutes of Medicine, Boston, MA 02115, United States.
2
Laboratory for Experimental Alzheimer Drugs (LEAD), Center for Neurologic Diseases, Harvard Medical School and Brigham and Women's Hospital, 77 Avenue Louis Pasteur, Harvard Institutes of Medicine, Boston, MA 02115, United States. Electronic address: caugelli-szafran@southernresearch.org.

Abstract

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

KEYWORDS:

Alzheimer’s disease; Aβ production; Notch-processing; γ-Amino alcohols; γ-Secretase inhibitors

PMID:
27020305
DOI:
10.1016/j.bmcl.2016.03.042
[Indexed for MEDLINE]

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