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Fukunaga K.,Mitsubishi Group | Sakai D.,Mitsubishi Group | Watanabe K.,Mitsubishi Group | Nakayama K.,Mitsubishi Group | And 13 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

We herein describe the results of further evolution of GSK-3β inhibitors for Alzheimer's disease from our promising compounds with in vivo tau phosphorylation inhibitory activity by oral administration. Introduction of a low alkyl group instead of the phenyl group at the 3-position of the morpholine moiety aiming to improve pharmacokinetic profiles resulted in potent low molecular weight GSK-3β inhibitors with good in vitro pharmacokinetic profiles, which also showed in vivo tau phosphorylation inhibitory activity by oral administration. Effect of the stereochemistry of the alkyl moiety is also discussed using docking models. © 2015 Elsevier Ltd. All rights reserved.

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