Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives

Rong Sheng; Yu Xu; Chunqi Hu; Jing Zhang; Xiao Lin; Jingya Li; Bo Yang; Qiaojun He; Yongzhou Hu

doi:10.1016/j.ejmech.2008.03.003

Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives

Eur J Med Chem. 2009 Jan;44(1):7-17. doi: 10.1016/j.ejmech.2008.03.003. Epub 2008 Mar 16.

Authors

Rong Sheng¹, Yu Xu, Chunqi Hu, Jing Zhang, Xiao Lin, Jingya Li, Bo Yang, Qiaojun He, Yongzhou Hu

Affiliation

¹ ZJU-ENS joint laboratory of Medicinal Chemistry, School of Pharmaceutical Sciences, Zijingang Campus, Zhejiang University Hangzhou 310058, People's Republic of China.

PMID: 18436348
DOI: 10.1016/j.ejmech.2008.03.003

Abstract

A new series of indanone and aurone derivatives have been synthesized and tested for in vitro AChE inhibitory activity by modified Ellman method. Most of them exhibit AChE inhibitory activities superior to rivastigmine. Further, the most potent compound 1g was selected to evaluate the effect on the acquisition and memory impairment by mice step-down passive avoidance test.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Benzofurans / chemical synthesis*
Benzofurans / pharmacology
Cholinesterase Inhibitors / chemical synthesis*
Cholinesterase Inhibitors / pharmacology
Drug Design
Indans / chemical synthesis*
Indans / pharmacology
Memory / drug effects
Mice
Pain / metabolism
Structure-Activity Relationship

Substances

Benzofurans
Cholinesterase Inhibitors
Indans
aurone
indacrinone