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Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.

Abstract：

:A new series of flavonoid derivatives have been designed, synthesized and evaluated as potent AChE inhibitors. Most of them showed more potent inhibitory activities to AChE than rivastigmine. The most potent inhibitor isoflavone derivative 10d inhibit AChE with a IC(50) of 4 nM and showed high BChE/AChE inhibition ratio (4575-fold), superior to donepezil (IC(50)=12 nM, 389-fold). Molecular docking studies were also performed to explore the detailed interaction with AChE.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Sheng R,Lin X,Zhang J,Chol KS,Huang W,Yang B,He Q,Hu Y

doi

10.1016/j.bmc.2009.07.072

subject

Has Abstract

pub_date

2009-09-15 00:00:00

pages

6692-8

issue

18

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00718-4

journal_volume

17

pub_type

杂志文章

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