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
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- 作者：Sumihiro Nomura ; Shigeki Sakamaki ; Mitsuya Hongu ; Eiji Kawanishi ; Yuichi Koga ; Toshiaki Sakamoto ; Yasuo Yamamoto ; Kiichiro Ueta ; Hirotaka Kimata ; Keiko Nakayama ; Minoru Tsuda-Tsukimoto
- 刊名：Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：September 9, 2010
- 年：2010
- 卷：53
- 期：17
- 页码：6355-6360
- 全文大小：806K
- 年卷期：v.53,no.17(September 9, 2010)
- ISSN：1520-4804
文摘
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.