Abstract
In order to investigate structure-activity relationships of azasugar series toward metalloproteinases, we synthesized and evaluated several azasugar-based compounds. As a result, it was found that 4-phenoxybenzene derivative 3 having 2R,3R,4R,5S-configurations exhibited most potent inhibitory activities against matrix metalloproteinase-1, -3 and -9 and TACE.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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ADAM Proteins
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ADAM17 Protein
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Aza Compounds / chemical synthesis*
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Aza Compounds / pharmacology
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Benzoates / chemistry
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Drug Design
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Gluconates / chemistry*
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Kinetics
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Lactones
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Matrix Metalloproteinase Inhibitors*
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Metalloendopeptidases / antagonists & inhibitors*
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Phenyl Ethers / chemistry
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Aza Compounds
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Benzoates
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Gluconates
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Lactones
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Matrix Metalloproteinase Inhibitors
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Phenyl Ethers
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Protease Inhibitors
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4-carboxybiphenyl ether
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ADAM Proteins
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Metalloendopeptidases
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ADAM17 Protein
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beta-glucono-1,5-lactone