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

2009; Elsevier BV; Volume: 17; Issue: 18 Linguagem: Inglês

10.1016/j.bmc.2009.07.072

1464-3391

Rong Sheng, Xiao Lin, Jing Zhang, Kim Sun Chol, Wenhai Huang, Bo Yang, Qiaojun He, Yongzhou Hu,

Phosphodiesterase function and regulation

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 IC50 of 4 nM and showed high BChE/AChE inhibition ratio (4575-fold), superior to donepezil (IC50 = 12 nM, 389-fold). Molecular docking studies were also performed to explore the detailed interaction with AChE.