Discovery of non-glucoside SGLT2 inhibitors

  • Bioorg Med Chem Lett. 2011 Apr 15;21(8):2472-5. doi: 10.1016/j.bmcl.2011.02.056.
An-Rong Li  1 ,  Jian Zhang ,  Joanne Greenberg ,  TaeWeon Lee ,  Jiwen Liu
Affiliations
  • 1. Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. [email protected]
PMID: 21398124 DOI: 10.1016/j.bmcl.2011.02.056
Abstract

A series of benzothiazinone and benzooxazinone derivatives were discovered as SGLT2 inhibitors. The optimization led to the discovery of compounds 31 and 32, which exhibited similar potency and better SGLT1 selectivity compared to dapagliflozin. These compounds may provide novel promising scaffolds, which are different from phlorizin-based SGLT2 inhibitors.