Abstract
A series of kojic acid (5-hydroxy-2-hydroxymethyl-4H-pyran-4-one) derivatives were synthesized and tested for their ability to inhibit D-amino acid oxidase (DAAO). Various substituents were incorporated into kojic acid at its 2-hydroxymethyl group. These analogs serve as useful molecular probes to explore the secondary binding site, which can be exploited in designing more potent DAAO inhibitors.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites / drug effects
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D-Amino-Acid Oxidase / antagonists & inhibitors*
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D-Amino-Acid Oxidase / metabolism
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Models, Molecular
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Molecular Probes / chemical synthesis
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Molecular Probes / chemistry
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Molecular Probes / pharmacology*
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Molecular Structure
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Pyrones / chemical synthesis
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Pyrones / chemistry
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Pyrones / pharmacology*
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Molecular Probes
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Pyrones
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kojic acid
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D-Amino-Acid Oxidase