Abstract
Ring opening of allobetulone gave either seco-acid 8 or di-acid 4. These acids were converted into esters that were screened by Ellman's assay. A dibutenylester of low cytotoxicity (NIH 3T3 murine embryonic fibroblasts) was shown to be a good mixed-type inhibitor (Ki=3.39, Ki'=2.26μM) for acetylcholinesterase.
Keywords:
Acetylcholinesterase inhibitor; Allobetulin; Alzheimer’s disease; Triterpene.
Copyright © 2015 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 / metabolism
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Alzheimer Disease / drug therapy
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Animals
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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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Humans
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Kinetics
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Mice
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NIH 3T3 Cells
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Structure-Activity Relationship
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Triterpenes / chemical synthesis
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Triterpenes / chemistry*
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Triterpenes / pharmacology*
Substances
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Cholinesterase Inhibitors
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Triterpenes
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betulin
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Acetylcholinesterase