Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents.

Abstract

A series of novel indanone derivatives was designed, synthesised and evaluated as potential agents for Alzheimer's disease. Among them, compound 6a, with a piperidine group linked to indone by a two-carbon spacer, exhibited the most potent inhibitor activity, with an IC(50) of 0.0018 μM for AChE; the inhibitory activity of this compound was 14-fold more potent than that of donepezil. Furthermore, these compounds also exhibited good metal-chelating ability.

• Authors: Fan-Chao Meng, Fei Mao, Wen-Jun Shan, Fangfei Qin, Ling Huang, Xing-Shu Li
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 22 Issue 13 Pg. 4462-6 (Jul 01 2012) ISSN: 1464-3405 [Electronic] England
• PMID: 22633691 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Ltd. All rights reserved.

Chemical References

• Chelating Agents
• Cholinesterase Inhibitors
• Indans
• Metals
• Pyridines
• indacrinone
• Acetylcholinesterase

Topics

• Acetylcholinesterase (chemistry, metabolism)
• Alzheimer Disease (drug therapy)
• Chelating Agents (chemical synthesis, chemistry, therapeutic use)
• Cholinesterase Inhibitors (chemical synthesis, chemistry, therapeutic use)
• Drug Design
• Humans
• Indans (chemical synthesis, chemistry, therapeutic use)
• Kinetics
• Metals (chemistry)
• Pyridines (chemical synthesis, chemistry, therapeutic use)
• Structure-Activity Relationship