1307845-14-2Relevant academic research and scientific papers
Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors
Du, Xiaohui,Lizarzaburu, Mike,Turcotte, Simon,Lee, Taeweon,Greenberg, Joanne,Shan, Bei,Fan, Peter,Ling, Yun,Medina, Julio C.,Houze, Jonathan
, p. 3774 - 3779 (2011/08/06)
Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharmacokinetic properties of this series of SGLT2 inhibitors. From these efforts, compounds 28 and 32 have improved solubility and pharmacokinetic properties compared to compound 1.
Discovery of non-glucoside SGLT2 inhibitors
Li, An-Rong,Zhang, Jian,Greenberg, Joanne,Lee, Taeweon,Liu, Jiwen
, p. 2472 - 2475 (2011/05/15)
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.
