Abstract
Novel thiophene C-aryl glucoside SGLT2 inhibitors were designed and synthesized. Two different types of thiophene derivatives were readily prepared. Among the compounds tested, ethylphenyl at the distal ring 71p showed the best in vitro inhibitory activity in this series to date (IC(50)=4.47 nM) against SGLT2.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Benzhydryl Compounds
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Glucosides / chemical synthesis
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Glucosides / chemistry*
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Glucosides / pharmacology
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Hypoglycemic Agents / chemical synthesis
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Hypoglycemic Agents / chemistry*
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Hypoglycemic Agents / pharmacology
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Sodium-Glucose Transporter 2 / metabolism
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Sodium-Glucose Transporter 2 Inhibitors*
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Structure-Activity Relationship
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Thiophenes / chemical synthesis
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Thiophenes / chemistry*
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Thiophenes / pharmacology
Substances
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(2R,3R,4S,5S,6R)-2-(5-chloro-4-(4-ethylbenzyl)thiophen-2-yl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol
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Benzhydryl Compounds
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Glucosides
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Hypoglycemic Agents
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Sodium-Glucose Transporter 2
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Sodium-Glucose Transporter 2 Inhibitors
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Thiophenes
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dapagliflozin