Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus (1)

Sumihiro Nomura, Shigeki Sakamaki, Mitsuya Hongu, Eiji Kawanishi, Yuichi Koga, Toshiaki Sakamoto, Yasuo Yamamoto, Kiichiro Ueta, Hirotaka Kimata, Keiko Nakayama, Minoru Tsuda-Tsukimoto

Research output: Contribution to journalArticle

236 Citations (Scopus)

Abstract

We discovered that C-glucosides 4 bearing a heteroaromatic ring formed metabolically more stable inhibitors for sodium-dependent glucose cotransporter 2 (SGLT2) than the O-glucoside, 2 (T-1095). A novel thiophene derivative 4b-3 (canagliflozin) was a highly potent and selective SGLT2 inhibitor and showed pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice.

Original languageEnglish
Pages (from-to)6355-6360
Number of pages6
JournalJournal of Medicinal Chemistry
Volume53
Issue number17
DOIs
Publication statusPublished - Sep 9 2010
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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