Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2016 May 1;26(9):2138-41. doi: 10.1016/j.bmcl.2016.03.077. Epub 2016 Mar 23.

Part 3: Notch-sparing γ-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones.

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

In search for novel lead compounds as γ-secretase inhibitors, analogs of aminopyrido[2,3-d]pyrimidin-7-ones (I) were synthesized and evaluated for inhibitory effects on amyloid-β-peptide production and cleavage of the Notch1 receptor mediated by γ-secretase. Selected pyridopyrimidines, such as 1, 8, 9, 10, 11 and 16 are γ-secretase inhibitors that did not have an effect on Notch1 receptor processing.

KEYWORDS:

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

PMID:
27038496
DOI:
10.1016/j.bmcl.2016.03.077
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center