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

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.
Baihua Xu 1 Yan Feng Binhua Lv Ge Xu Lili Zhang Jiyan Du Kun Peng Min Xu Jiajia Dong Wenbin Zhang Ting Zhang Liangcheng Zhu Haifeng Ding Zelin Sheng Ajith Welihinda Brian Seed Yuanwei Chen
Affiliations

Affiliation

  • 1 Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, Sichuan 610041, PR China. xubaihua2002@126.com
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.

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