Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors

Rong Sheng; Xiao Lin; Jingya Li; Yanke Jiang; Zhicai Shang; Yongzhou Hu

doi:10.1016/j.bmcl.2005.05.132

Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3834-7. doi: 10.1016/j.bmcl.2005.05.132.

Authors

Rong Sheng¹, Xiao Lin, Jingya Li, Yanke Jiang, Zhicai Shang, Yongzhou Hu

Affiliation

¹ ZJU-ENS Joint Laboratory of Medicinal Chemistry, Zhejiang University, Hubin Campus, Hangzhou 310031,China.

PMID: 15993600
DOI: 10.1016/j.bmcl.2005.05.132

Abstract

A series of 2-phenoxy-indan-1-one derivatives have been designed, synthesized, and tested as acetylcholinesterase inhibitors. The most potent compound exhibited high AChE inhibitory activity (IC50 = 50 nM), and the molecular docking study indicated that it was nicely accommodated by AChE.

Publication types

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

MeSH terms

Acetylcholinesterase / chemistry
Animals
Cerebral Cortex / metabolism
Cholinesterase Inhibitors / chemical synthesis*
Cholinesterase Inhibitors / pharmacology
Drug Design
Indans / chemical synthesis*
Indans / pharmacology
Inhibitory Concentration 50
Ketones
Models, Molecular
Protein Binding
Rats
Structure-Activity Relationship

Substances

Cholinesterase Inhibitors
Indans
Ketones
Acetylcholinesterase