2. Academic Validation
  3. Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors

Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors

  • Bioorg Med Chem Lett. 2009 Dec 15;19(24):6877-81. doi: 10.1016/j.bmcl.2009.10.088.
Binhua Lv 1,  Baihua Xu,  Yan Feng,  Kun Peng,  Ge Xu,  Jiyan Du,  Lili Zhang,  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 610041, PR China. 51popo51@163.com
PMID: 19896374 DOI: 10.1016/j.bmcl.2009.10.088
Abstract

A series of novel O-spiroketal C-arylglucosides have been prepared and evaluated in cell-based functional assays for activity against human sodium-dependent glucose co-transporters 1 and 2 (SGLT1 and 2). The core spiro[isobenzofuran-1,2'-pyran] structure proved to be an effective scaffold for diversification and a number of compounds with single digit nanomolar potency and high selectivity have been synthesized. Compound 5a promoted glucosuria when administered in vivo in rats and produced a significant blood glucose reduction effect.

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