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

doi:10.1248/cpb.c13-00407

Regular Articles

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

著者情報

Shigeki Sakamaki
Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation
Eiji Kawanishi
Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation
Yuichi Koga
Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation
Yasuo Yamamoto
Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation
Chiaki Kuriyama
Pharmacology Research Laboratories, Mitsubishi Tanabe Pharma Corporation
Yasuaki Matsushita
Pharmacology Research Laboratories, Mitsubishi Tanabe Pharma Corporation
Kiichiro Ueta
Pharmacology Research Laboratories, Mitsubishi Tanabe Pharma Corporation
Sumihiro Nomura 責任著者
Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation

キーワード: sodium-dependent glucose cotransporter, glucal-boronate, thiophene-C-glucoside

ジャーナルフリー HTML

2013 年 61 巻 10 号 p. 1037-1043

DOI https://doi.org/10.1248/cpb.c13-00407

詳細

抄録

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.

責任著者(Corresponding author)

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