Discovery of ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor …

…, R Shiraki, T Ogiyama, T Murakami, E Kurosaki…

文献索引：Imamura, Masakazu; Nakanishi, Keita; Suzuki, Takayuki; Ikegai, Kazuhiro; Shiraki, Ryota; Ogiyama, Takashi; Murakami, Takeshi; Kurosaki, Eiji; Noda, Atsushi; Kobayashi, Yoshinori; Yokota, Masayuki; Koide, Tomokazu; Kosakai, Kazuhiro; Ohkura, Yasufumi; Takeuchi, Makoto; Tomiyama, Hiroshi; Ohta, Mitsuaki Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 10 p. 3263 - 3279

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被引用次数: 58

摘要

A series of C-glucosides with various heteroaromatics has been synthesized and its inhibitory activity toward SGLTs was evaluated. Upon screening several compounds, the benzothiophene derivative (14a) was found to have potent inhibitory activity against SGLT2 and good selectivity versus SGLT1. Through further optimization of 14a, a novel benzothiophene derivative (14h; ipragliflozin, ASP1941) was discovered as a highly ...