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

  • Meng F
  • Mao F
  • Shan W
 et al. 
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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 IC50of 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. © 2012 Elsevier Ltd. All rights reserved.

Author-supplied keywords

  • Acetylcholinesterase inhibitors
  • Alzheimer's disease
  • Indanone derivatives
  • Metal-chelating agents

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