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Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents.

Abstract：

:A new series of 4-dimethylamine flavonoid derivatives were designed and synthesized as potential multifunctional anti-Alzheimer agents. The inhibition of cholinesterase activity, self-induced β-amyloid (Aβ) aggregation, and antioxidant activity by these derivatives was investigated. Most of the compounds exhibited potent acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. A Lineweaver-Burk plot and molecular modeling study showed that these compounds targeted both the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. The derivatives showed potent self-induced Aβ aggregation inhibition and peroxyl radical absorbance activity. Moreover, compound 6d significantly protected PC12 neurons against H2O2-induced cell death at low concentrations. Thus, these compounds could become multifunctional agents for further development for the treatment of AD.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Luo W,Wang T,Hong C,Yang YC,Chen Y,Cen J,Xie SQ,Wang CJ

doi

10.1016/j.ejmech.2016.06.022

subject

Has Abstract

pub_date

2016-10-21 00:00:00

pages

17-26

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30500-1

journal_volume

122

pub_type

杂志文章

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