Discovery of Canagliflozin, a Novel <i>C</i>-Glucoside with Thiophene Ring, as Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes Mellitus
Sumihiro Nomura(Mitsubishi Corporation (United States)), Shigeki Sakamaki(Mitsubishi Chemical (Japan)), Mitsuya Hongu(Mitsubishi Corporation (United States)), Eiji Kawanishi(Mitsubishi Corporation (United States)), Yuichi Koga(Mitsubishi Corporation (United States)), Toshiaki Sakamoto(Mitsubishi Corporation (United States)), Yasuo Yamamoto(Mitsubishi Chemical (Japan)), Kiichiro Ueta(Pharmacology Research Institute), Hirotaka Kimata(Pharmacology Research Institute), Keiko Nakayama(Pharmacology Research Institute), Minoru Tsuda-Tsukimoto(Mitsubishi Corporation (United States))
Cited by 376Open Access
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.
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