Publication | Open Access
Synthesis and Biological Evaluation of Thiophene-<i>C</i>-glucosides as Sodium-Dependent Glucose Cotransporter 2 Inhibitors
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2013
Year
Molecular PharmacologyMedicinal ChemistryPharmaceutical ScienceRemarkable Inhibitory ActivityBiochemistryMedicineNatural SciencesChlorothiophene Derivative 3FStructure-activity RelationshipCellular PharmacologyBiological EvaluationDrug DevelopmentPharmacologyMolecular ModelingPharmaceutical ChemistryInhibitory ActivityDrug DiscoveryNatural Product Synthesis
The synthesis and structure-activity relationship (SAR) of thiophene-C-glucosides have been explored, and the human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitory activities and rat urinary glucose excretion (UGE) effects of 3a-f were evaluated. As a result, they showed good hSGLT2 inhibitory activities and rat UGE effects. In particular, the chlorothiophene derivative 3f showed remarkable inhibitory activity against hSGLT2.
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