ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.

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Xu B, Feng Y, Lv B, Xu G, Zhang L, Du J, Peng K, Xu M, Dong J, Zhang W, Zhang T, Zhu L, Ding H, Sheng Z, Welihinda A, Seed B, Chen Y

ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.

Bioorg Med Chem. 2010 Jun 15;18(12):4422-32. doi: 10.1016/j.bmc.2010.04.088. Epub 2010 Apr 29.

PubMed ID

20576578 [ View in PubMed

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Abstract

A series of 2-substituted C-aryl glucosides have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of an appropriate ortho substituent at the proximal phenyl ring adjacent to the glycosidic bond was found to improve SGLT2 inhibitory activity and dramatically increase selectivity for hSGLT2 over hSGLT1. Selected compounds were investigated for in vivo efficacy.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dapagliflozin	Sodium/glucose cotransporter 2	IC 50 (nM)	6.7	N/A	N/A	Details