Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors

Novel C-aryl glucoside SGLT2 inhibitors containing pyrimidine motif were designed and synthesized for biological evaluation. Among the compounds assayed, pyrimidine containing methylthio moiety 11g demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date (IC50 = 10.7 nM).

Graphical abstractNovel C-aryl glucoside SGLT2 inhibitors containing pyrimidine motif were designed and synthesized for biological evaluation. Among various analogs tested, methylthiopyrimidine 11g demonstrated best in vitro activity against hSGLT2 in this series to date.Figure optionsDownload full-size imageDownload as PowerPoint slide