2. Academic Validation
  3. C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes

C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes

  • Bioorg Med Chem Lett. 2011 Aug 1;21(15):4465-70. doi: 10.1016/j.bmcl.2011.06.032.
Baihua Xu 1,  Yan Feng,  Huawei Cheng,  Yanli Song,  Binhua Lv,  Yuelin Wu,  Congna Wang,  Shengbin Li,  Min Xu,  Jiyan Du,  Kun Peng,  Jiajia Dong,  Wenbin Zhang,  Ting Zhang,  Liangcheng Zhu,  Haifeng Ding,  Zelin Sheng,  Ajith Welihinda,  Jacques Y Roberge,  Brian Seed,  Yuanwei Chen
Affiliations

Affiliation

  • 1 Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, Sichuan, PR China. baihuaxu@egretpharma.com
PMID: 21737266 DOI: 10.1016/j.bmcl.2011.06.032
Abstract

A series of C-aryl glucosides with various substituents at the 4'-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of alkyl or alkoxy substituents at the 4'-position was found to improve SGLT2 potency, whereas introduction of a hydrophilic group at this position was deleterious. Compounds with alkoxy-, cycloalkoxy- or cycloalkenyloxy-ethoxy scaffolds exhibited good inhibitory activity and high selectivity toward SGLT2. Selected compounds were investigated for in vivo efficacy.

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