C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.

@article{Robinson2010CArylGI,
  title={C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.},
  author={Ralph P Robinson and Vincent Mascitti and Carine M. Boustany-Kari and Christopher L. Carr and Patrick M Foley and Emi Kimoto and Michael T. Leininger and Andr{\'e} Lowe and Michelle K Klenotic and James I Macdonald and Robert J. Maguire and Victoria M Masterson and Tristan S. Maurer and Zhuang Miao and Jigna D. Patel and Cathy Pr{\'e}ville and Matthew R Reese and Li She and Claire M. Steppan and Benjamin A Thuma and Tong Zhu},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 5},
  pages={1569-72}
}
Modifications to the sugar portion of C-aryl glycoside sodium glucose transporter 2 (SGLT2) inhibitors were explored, including systematic deletion and modification of each of the glycoside hydroxyl groups. Based on results showing activity to be quite tolerant of structural change at the C-5 position, a series of novel C-5 spiro analogues was prepared. Some of these analogues exhibit low nanomolar potency versus SGLT2 and promote urinary glucose excretion (UGE) in rats. However, due to sub… CONTINUE READING