Abstract
In order to investigate SAR regarding proximal phenyl ring in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on proximal phenyl ring was conducted. During a series of lead optimization efforts, ortho-allyloxyphenyl 10p or ortho-hydroxyphenyl 11a showed subnanomolar inhibitory activity against hSGLT2.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
MeSH terms
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Animals
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Biological Transport / drug effects
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CHO Cells
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Carbon Radioisotopes
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Cricetulus
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Gene Expression
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Glucosides / chemical synthesis*
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Glucosides / pharmacology
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Humans
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / pharmacology
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Methylglucosides / metabolism
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Recombinant Proteins / chemistry
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Small Molecule Libraries / chemical synthesis*
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Small Molecule Libraries / pharmacology
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Sodium-Glucose Transporter 2 / chemistry
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Sodium-Glucose Transporter 2 Inhibitors*
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology
Substances
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Carbon Radioisotopes
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Glucosides
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Hypoglycemic Agents
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Methylglucosides
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Recombinant Proteins
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SLC5A2 protein, human
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Small Molecule Libraries
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Sodium-Glucose Transporter 2
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Sodium-Glucose Transporter 2 Inhibitors
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Thiazoles