TY - JOUR
T1 - Synthesis and biological evaluation of thiophene-C-glucosides as sodium-dependent glucose cotransporter 2 inhibitors
AU - Sakamaki, Shigeki
AU - Kawanishi, Eiji
AU - Koga, Yuichi
AU - Yamamoto, Yasuo
AU - Kuriyama, Chiaki
AU - Matsushita, Yasuaki
AU - Ueta, Kiichiro
AU - Nomura, Sumihiro
N1 - Copyright:
Copyright 2013 Elsevier B.V., All rights reserved.
PY - 2013/10
Y1 - 2013/10
N2 - 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.
AB - 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.
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U2 - 10.1248/cpb.c13-00407
DO - 10.1248/cpb.c13-00407
M3 - Article
C2 - 24088695
AN - SCOPUS:84886680185
SN - 0009-2363
VL - 61
SP - 1037
EP - 1043
JO - Chemical and Pharmaceutical Bulletin
JF - Chemical and Pharmaceutical Bulletin
IS - 10
ER -