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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).