Synthesis and biological evaluation of thieno[3,2–c]pyrazol-3-amine derivatives as potent glycogen synthase kinase 3β inhibitors for Alzheimer’s disease

Ning Yan,Fei Xie,Long-Qian Tang,De-Feng Wang,Xiang Li,Chao Liu,Zhao-Peng Liu

Bioorganic Chemistry（2023）

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摘要

•A potent GSK-3β inhibitor 54 (IC50 = 3.4 nM) was identified.•Compound 54 showed neuroprotective effects on Aβ1-42-induced neurotoxicity.•Compound 54 inhibited tau hyperphosphorylation.•Compound 54 inhibited LPS-induced iNOS expression.•Compound 54 improved AlCl3-induced dyskinesia in zebrafish.

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关键词

alzheimers,potent glycogen synthase kinase,inhibitors

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