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.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / chemistry*
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Acetylcholinesterase / metabolism
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Alzheimer Disease / drug therapy
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Chelating Agents / chemical synthesis*
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Chelating Agents / chemistry
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Chelating Agents / therapeutic use
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Cholinesterase Inhibitors / chemical synthesis*
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Cholinesterase Inhibitors / chemistry
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Cholinesterase Inhibitors / therapeutic use
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Drug Design*
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Humans
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Indans / chemical synthesis*
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Indans / chemistry
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Indans / therapeutic use
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Kinetics
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Metals / chemistry*
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / therapeutic use
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Structure-Activity Relationship
Substances
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Chelating Agents
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Cholinesterase Inhibitors
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Indans
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Metals
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Pyridines
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indacrinone
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Acetylcholinesterase