Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer’s Disease

[Image: see text] An exploration of the SAR of the side chain of a novel tricyclic series of γ-secretase inhibitors led to the identification of compound (−)-16 (SCH 900229), which is a potent and PS1 selective inhibitor of γ-secretase (Aβ40 IC(50) = 1.3 nM). Compound (−)-16 demonstrated excellent l...

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Hauptverfasser: Wu, Wen-Lian, Domalski, Martin, Burnett, Duane A., Josien, Hubert, Bara, Thomas, Rajagopalan, Murali, Xu, Ruo, Clader, John, Greenlee, William J., Brunskill, Andrew, Hyde, Lynn A., Del Vecchio, Robert A., Cohen-Williams, Mary E., Song, Lixin, Lee, Julie, Terracina, Giuseppe, Zhang, Qi, Nomeir, Amin, Parker, Eric M., Zhang, Lili
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2012
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4025742/
https://ncbi.nlm.nih.gov/pubmed/24900404
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml300044f
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