Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin

[Display omitted] Herein we describe design strategies that led to the discovery of novel pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) incorporating an indole motif as a heterocyclic replacement for a naphthyl moiety that was present in the original lead 9. Tactics involving parallel medic...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-02, Vol.25 (4), p.908-913
Hauptverfasser:	Pettersson, Martin, Johnson, Douglas S., Humphrey, John M., am Ende, Christopher W., Evrard, Edelweiss, Efremov, Ivan, Kauffman, Gregory W., Stepan, Antonia F., Stiff, Cory M., Xie, Longfei, Bales, Kelly R., Hajos-Korcsok, Eva, Murrey, Heather E., Pustilnik, Leslie R., Steyn, Stefanus J., Wood, Kathleen M., Verhoest, Patrick R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer’s disease Amyloid Precursor Protein Secretases - drug effects Animals Drug Discovery Indoles - chemistry Indoles - pharmacology Presenilins - drug effects Pyrazines - chemistry Rats γ-Secretase modulators
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