Chemical Research in Chinese Universities ›› 2017, Vol. 33 ›› Issue (4): 594-597.doi: 10.1007/s40242-017-6462-x

• Articles • Previous Articles     Next Articles

Synthesis and Acetylcholinesterase Inhibitory Activity of Polymethoxyflavone Mannich Base Derivatives

SHI Ling, ZHANG Yanhua, WANG Caifang, LIU Haoran, WANG Qiuan   

  1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, P. R. China
  • Received:2016-11-23 Revised:2017-02-10 Online:2017-08-01 Published:2017-07-19
  • Contact: WANG Qiuan E-mail:wangqa@hnu.edu.cn
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.J1210040) and the Hunan Provincial Natural Science Foundation,China(No.14JJ2048).

Abstract:

A series of novel polymethoxyflavone Mannich base derivatives 1-8 was synthesized by Mannich reaction of 5-hydroxy-3,7,3',4'-tetramethoxyflavone 9 with various secondary aliphatic amines and formaldehyde. Their acetylcholinesterase(AChE) inhibitory activities were evaluated. The results showed that most of them exhibited AChE inhibitory activity and especially piperidin-1-yl methyl substituent derivative 5(IC50=0.238 μmol/L) demonstrated stronger activity comparable with the positive control, neoeserinemethyl sulfate(IC50=1.39 μmol/L), which is worthy of further development as an agent for Alzheimer's disease treatment.

Key words: Polymethoxyflavone, Mannich base derivative, Acetylcholinesterase inhibitory activity