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

abstract

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

authors

• Lu, Dai

published proceedings

• Bioorg Med Chem Lett

altmetric score

• 15.5

author list (cited authors)

• Zhang, J., Lu, D., Wei, H., Gu, Y., Selkoe, D. J., Wolfe, M. S., & Augelli-Szafran, C. E.

citation count

• 2

complete list of authors

• Zhang, Jing||Lu, Dai||Wei, Han-Xun||Gu, Yongli||Selkoe, Dennis J||Wolfe, Michael S||Augelli-Szafran, Corinne E

publication date

• January 2016

publisher

• Elsevier  Publisher

published in

• Bioorganic and Medicinal Chemistry Letters  Journal

keywords

• Alzheimer’s Disease
• Aminopyridopyrimidines
• Amyloid Beta-Peptides
• Amyloid Precursor Protein Secretases
• Animals
• Aβ Production
• Humans
• Microsomes, Liver
• Notch-processing
• Peptide Fragments
• Protease Inhibitors
• Pyridones
• Pyrimidines
• Rats
• Receptor, Notch1
• Structure-Activity Relationship
• γ-secretase Inhibitors

Digital Object Identifier (DOI)

• 10.1016/j.bmcl.2016.03.077

start page

• 2138

end page

• 2141

volume

• 26

issue

• 9

URL

• http://dx.doi.org/10.1016/j.bmcl.2016.03.077