Synthesis and biological evaluation of novel flavonoid derivatives as dual binding acetylcholinesterase inhibitors.

@article{Shen2009SynthesisAB,
  title={Synthesis and biological evaluation of novel flavonoid derivatives as dual binding acetylcholinesterase inhibitors.},
  author={Yanhong Shen and Jing Zhang and Rong W Sheng and Xiao-Wu Dong and Qiaojun He and Bo Yang and Yongzhou Hu},
  journal={Journal of enzyme inhibition and medicinal chemistry},
  year={2009},
  volume={24 2},
  pages={372-80}
}
A new series of flavonoid derivatives have been designed, synthesised and evaluated as acetylcholinesterase inhibitors that could bind simultaneously to the peripheral and catalytic sites of the enzyme. Among them, fifteen derivatives were found to inhibit the enzyme in the micromolar range and isoflavone derivatives possessed more potent inhibitory activity than other flavonoid derivatives. The best compound 9a had its inhibitory activity (IC(50) = 0.093 microM) in the same range as the… CONTINUE READING

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