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

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.

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