N-glucosides as human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitors

Yasuo Yamamoto, Eiji Kawanishi, Yuichi Koga, Shigeki Sakamaki, Toshiaki Sakamoto, Kiichiro Ueta, Yasuaki Matsushita, Chiaki Kuriyama, Minoru Tsuda-Tsukimoto, Sumihiro Nomura

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)


Inhibition of renal sodium-dependent glucose cotransporter 2 (SGLT2) increases urinary glucose excretion (UGE), and thus reduces blood glucose levels in hyperglycemia. A series of N-glucosides was synthesized for biological evaluation as human SGLT2 (hSGLT2) inhibitors. Among these compounds, N-glucoside 9d possessing an indole core structure showed good in vitro activity (IC50 = 7.1 nM against hSGLT2). Furthermore, 9d exhibited favorable in vivo potency with regard to UGE in rats based on good pharmacokinetic profiles.

Original languageEnglish
Pages (from-to)5641-5645
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
Publication statusPublished - Oct 15 2013
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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