2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: A study on the importance of modifications at the side chain on the activity
作者:Yanhong Shen、Rong Sheng、Jing Zhang、Qiaojun He、Bo Yang、Yongzhou Hu
DOI:10.1016/j.bmc.2008.07.014
日期:2008.8
As a part of our project aimed at developing new agents of potential application in AD, a new series of 2-phenoxy-indan-1-one derivatives which possess alkylamine side chain were designed, synthesized and evaluated for their inhibitory activity against AChE and BuChE. Most of the compounds were found to inhibit AChE in the nanomolar range. The optimum inhibitor 3g exhibited 34-fold increase in AChE inhibition than donepezil and displayed neuroprotective effect against H2O2-induced cell death. (C) 2008 Elsevier Ltd. All rights reserved.