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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Publicat a:ACS Med Chem Lett
Autors principals: 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.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2015
Accés en línia: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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