Abstract
A new series of flavonoid derivatives have been designed, synthesized and evaluated as potent AChE inhibitors. Most of them showed more potent inhibitory activities to AChE than rivastigmine. The most potent inhibitor isoflavone derivative 10d inhibit AChE with a IC(50) of 4 nM and showed high BChE/AChE inhibition ratio (4575-fold), superior to donepezil (IC(50)=12 nM, 389-fold). Molecular docking studies were also performed to explore the detailed interaction with AChE.
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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Animals
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Binding Sites
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Butyrylcholinesterase / chemistry
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Butyrylcholinesterase / metabolism
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Cholinesterase Inhibitors / chemical synthesis
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Cholinesterase Inhibitors / chemistry*
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Cholinesterase Inhibitors / pharmacology*
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Computer Simulation
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Flavonoids / chemical synthesis
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Flavonoids / chemistry*
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Flavonoids / pharmacology*
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Inhibitory Concentration 50
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Models, Molecular
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Molecular Structure
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Phenylcarbamates / pharmacology
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Protein Binding
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Rats
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Rivastigmine
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Structure-Activity Relationship
Substances
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Cholinesterase Inhibitors
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Flavonoids
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Phenylcarbamates
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Acetylcholinesterase
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Butyrylcholinesterase
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Rivastigmine