Abstract
O-glucuronides and O-glucosides of a series of pyrazoles analogues were synthesized and evaluated for their SGLT inhibitory activity in brush border membrane vehicles (BBMVs) of rat kidney. O-glucosides of certain pyrazole analogues inhibited the transport of [(14)C]-glucose in BBMVs, and induced glucosuria in Wistar rats by intravenous injection.
MeSH terms
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Animals
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Enzyme Inhibitors / administration & dosage
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Glucose / metabolism
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Glucosides / administration & dosage
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Glucosides / chemical synthesis*
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Glucosides / pharmacology*
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Glycosuria / chemically induced
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Glycosuria / metabolism
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Hypoglycemic Agents / administration & dosage
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / pharmacology*
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Indicators and Reagents
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Injections, Intravenous
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Kidney / drug effects
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Kidney / metabolism*
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Membrane Glycoproteins / antagonists & inhibitors*
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Microvilli / drug effects
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Microvilli / metabolism
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Monosaccharide Transport Proteins / antagonists & inhibitors*
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Pyrazoles / chemical synthesis
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Pyrazoles / pharmacology
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Rats
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Rats, Wistar
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Sodium-Glucose Transporter 1
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Glucosides
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Hypoglycemic Agents
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Indicators and Reagents
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Membrane Glycoproteins
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Monosaccharide Transport Proteins
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Pyrazoles
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Slc5a1 protein, rat
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Sodium-Glucose Transporter 1
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WAY 123783
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Glucose