Abstract
Monoamine oxidase-B (MAO-B) inhibitor has been used as neuroprotectants to treat the motor deficits of Parkinson's disease (PD). We designed and synthesized a class of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors. The compounds have various inhibitory effects, with compound 6a having a K(i) value of 0.26 μM. Their promising activity in vitro suggests potential use in the treatment of PD.
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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Amides / chemical synthesis
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Amides / chemistry
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Amides / pharmacology
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Animals
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology
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Cell Line
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Drug Design*
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Enzyme Activation / drug effects
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Humans
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Mice
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Molecular Structure
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Monoamine Oxidase Inhibitors / chemical synthesis*
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Monoamine Oxidase Inhibitors / pharmacology*
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Phenol / chemical synthesis
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Phenol / chemistry
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Phenol / pharmacology
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Purines / chemical synthesis*
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Purines / chemistry
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Purines / pharmacology
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Xanthines / chemical synthesis
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Xanthines / chemistry
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Xanthines / pharmacology
Substances
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(E)-2-styryl-1-methylbenzimidazole
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Amides
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Benzimidazoles
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Monoamine Oxidase Inhibitors
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Purines
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Xanthines
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istradefylline
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Phenol