Synthesis and biological evaluation of thiophene-C-glucosides as sodium-dependent glucose cotransporter 2 inhibitors

Shigeki Sakamaki, Eiji Kawanishi, Yuichi Koga, Yasuo Yamamoto, Chiaki Kuriyama, Yasuaki Matsushita, Kiichiro Ueta, Sumihiro Nomura

Research output: Contribution to journalArticle

13 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1037-1043
Number of pages7
JournalChemical and Pharmaceutical Bulletin
Volume61
Issue number10
DOIs
Publication statusPublished - Oct 1 2013
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Drug Discovery

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