Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability

[Image: see text] Herein we describe the design and synthesis of a series of pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) for Alzheimer’s disease (AD) that achieve good alignment of potency, metabolic stability, and low MDR efflux ratios, while also maintaining favorable physicochemical pr...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Pettersson, Martin, Johnson, Douglas S., Humphrey, John M., Butler, Todd W., am Ende, Christopher W., Fish, Benjamin A., Green, Michael E., Kauffman, Gregory W., Mullins, Patrick B., O’Donnell, Christopher J., Stepan, Antonia F., Stiff, Cory M., Subramanyam, Chakrapani, Tran, Tuan P., Vetelino, Beth Cooper, Yang, Eddie, Xie, Longfei, Bales, Kelly R., Pustilnik, Leslie R., Steyn, Stefanus J., Wood, Kathleen M., Verhoest, Patrick R.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4434474/
https://ncbi.nlm.nih.gov/pubmed/26005540
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00070
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