Design, synthesis, and evaluation of genipin derivatives for the treatment of Alzheimer's Disease | Zendy

Huang Weijun | Zendy; Wang Yujun | Zendy; Li Jiaming | Zendy; Zhang Yanchun | Zendy; Ma Xiaodong | Zendy; Zhu Panhu | Zendy; Zhang Yang | Zendy

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Design, synthesis, and evaluation of genipin derivatives for the treatment of Alzheimer's Disease

Author(s) -

Huang Weijun,

Wang Yujun,

Li Jiaming,

Zhang Yanchun,

Ma Xiaodong,

Zhu Panhu,

Zhang Yang

Publication year - 2019

Publication title -

chemical biology and drug design

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.59

H-Index - 77

eISSN - 1747-0285

pISSN - 1747-0277

DOI - 10.1111/cbdd.13194

Subject(s) - genipin , acetylcholinesterase , donepezil , moiety , chemistry , neuroprotection , β amyloid , inhibitory postsynaptic potential , mtt assay , aché , pharmacology , amyloid precursor protein , biochemistry , stereochemistry , alzheimer's disease , enzyme , in vitro , disease , medicine , dementia , chitosan

Twenty‐two novel genipin derivatives have been designed, synthesized, and evaluated for their inhibitory activity against acetylcholinesterase ( AC hE). As a result, compound 13a bearing ligustrazine moiety displayed the most potent AC hE inhibitory activity in this series with IC 50 value of 218 n m . Besides, MTT assay was performed to investigate the neuroprotection of these compounds against PC 12 cells injured by Amyloid β‐protein 1–42 (Aβ 1–42 ). Among them, 8a showed higher inhibition rate (%Inhibition = 22.29) than the positive reference Donepezil (%Inhibition = 17.65).

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