Development of Sodium-Dependent Glucose Co-Transporter 2 Inhibitors as Potential Anti-Diabetic Therapeutics

Author(s): Low-Tone Ho, Suvarn S. Kulkarni, Jinq-Chyi Lee

Journal Name: Current Topics in Medicinal Chemistry

Volume 11 , Issue 12 , 2011

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The kidney plays an important role in the regulation of plasma glucose. It is estimated that greater than 99% of the renal glucose filtered by kidney glomerulus is resorbed by sodium-dependent glucose co-transporters (SGLTs), and that SGLT2 located in the proximal renal tubule achieves the most of this assignment. Studies of SGLT2 inhibitors indicate that raising renal glucose excretion by inhibiting SGLT2 helps effectively normalize the plasma glucose levels in individuals with type 2 diabetes mellitus (T2DM). This review discusses the discovery of SGLT2 inhibitors and the related structure-activity relationship (SAR) studies. The clinical trial data of dapagliflozin is also involved.

Keywords: Dapagliflozin, phlorizin, sodium-dependent glucose co-transporter, structure-activity relationships, type 2 diabetes mellitus, regulation of plasma glucose, SGLT2 inhibitors, relatedstructure-activity relationship, insulin deficiency

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Article Details

Year: 2011
Page: [1476 - 1512]
Pages: 37
DOI: 10.2174/156802611795860915
Price: $65

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