O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors

  • Bioorg Med Chem Lett. 2009 Oct 1;19(19):5632-5. doi: 10.1016/j.bmcl.2009.08.030.
Baihua Xu  1 ,  Binhua Lv ,  Yan Feng ,  Ge Xu ,  Jiyan Du ,  Ajith Welihinda ,  Zelin Sheng ,  Brian Seed ,  Yuanwei Chen
Affiliations
  • 1. Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, Sichuan 610041, PR China. [email protected]
PMID: 19700318 DOI: 10.1016/j.bmcl.2009.08.030
Abstract

Two series of O-spiro C-aryl glucosides were synthesized and tested for inhibition of hSGLT1 and hSGLT2. 6'-O-Spiro C-aryl glucosides exhibited potent in vitro hSGLT2 inhibitory activity but 2'-O-spiro C-aryl glucosides showed no in vitro hSGLT2 inhibitory activity at a screening concentration of 1microM.