Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors |
| |
| Authors: | Rong Sheng Xiao Lin Jing Zhang Kim Sun Chol Wenhai Huang Bo Yang Qiaojun He Yongzhou Hu |
| |
| Affiliation: | aZJU-ENS Joint Laboratory of Medicinal Chemistry, School of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China;bDepartment of Pharmacology, School of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China;cDepartment of Chemistry, Pyongsong Medical University, Pyongsong, Democratic People’s Republic of Korea |
| |
| 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 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. |
| |
| Keywords: | Flavonoid derivatives Synthesis AChE inhibitor |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
