Synthesis and Biological Evaluation of Thiophene-C-glucosides as Sodium-Dependent Glucose Cotransporter 2 Inhibitors

Sakamaki, S; Kawanishi, E; Koga, Y; Yamamoto, Y; Kuriyama, C; Matsushita, Y; Ueta, K; Nomura, S

HERO ID

4947098

Reference Type

Journal Article

Year

2013

HERO ID 4947098
In Press No
Year 2013
Title Synthesis and Biological Evaluation of Thiophene-C-glucosides as Sodium-Dependent Glucose Cotransporter 2 Inhibitors
Authors Sakamaki, S; Kawanishi, E; Koga, Y; Yamamoto, Y; Kuriyama, C; Matsushita, Y; Ueta, K; Nomura, S
Journal Chemical and Pharmaceutical Bulletin
Volume 61
Issue 10
Page Numbers 1037-1043
Abstract The synthesis and structure-activity relationship (SAR) of thiophene-C-glucosides have been explored, and the human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitory activities and rat urinary glucose excretion (UGE) effects of 3a-f were evaluated. As a result, they showed good hSGLT2 inhibitory activities and rat UGE effects. In particular, the chlorothiophene derivative 3f showed remarkable inhibitory activity against hSGLT2.
Doi 10.1248/cpb.c13-00407
Wosid WOS:000326302300008
Is Certified Translation No
Dupe Override No
Is Public Yes
Keyword sodium-dependent glucose cotransporter; glucal-boronate; thiophene-C-glucoside