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Discovery of remogliflozin etabonate: A potent and highly selective SGLT2 inhibitor
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2021-01-22 , DOI: 10.1016/j.bmc.2021.116033 Kazuo Shimizu 1 , Hideki Fujikura 2 , Nobuhiko Fushimi 2 , Toshihiro Nishimura 2 , Kazuya Tatani 2 , Kenji Katsuno 2 , Yoshikazu Fujimori 2 , Shinjiro Watanabe 2 , Masahiro Hiratochi 2 , Takeshi Nakabayashi 2 , Noboru Kamada 2 , Koichi Arakawa 2 , Hidemasa Hikawa 3 , Isao Azumaya 3 , Masayuki Isaji 2
中文翻译：
发现 remogliflozin etabonate：一种有效且高度选择性的 SGLT2 抑制剂
更新日期：2021-02-11
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2021-01-22 , DOI: 10.1016/j.bmc.2021.116033 Kazuo Shimizu 1 , Hideki Fujikura 2 , Nobuhiko Fushimi 2 , Toshihiro Nishimura 2 , Kazuya Tatani 2 , Kenji Katsuno 2 , Yoshikazu Fujimori 2 , Shinjiro Watanabe 2 , Masahiro Hiratochi 2 , Takeshi Nakabayashi 2 , Noboru Kamada 2 , Koichi Arakawa 2 , Hidemasa Hikawa 3 , Isao Azumaya 3 , Masayuki Isaji 2
Affiliation
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We optimized the structure of an active metabolite (1) of WAY-123783, which was obtained from mouse urine after oral administration, to improve selectivity for SGLT2 and oral bioavailability. O-glucoside derivative 24 (remogliflozin etabonate) was subsequently identified as a potent, highly selective, and orally available SGLT2 inhibitor.
中文翻译：
发现 remogliflozin etabonate：一种有效且高度选择性的 SGLT2 抑制剂
我们优化了口服给药后从小鼠尿液中获得的 WAY-123783活性代谢物(1)的结构，以提高对 SGLT2 的选择性和口服生物利用度。O-葡萄糖苷衍生物24（remogliflozin etabonate）随后被鉴定为一种有效的、高选择性的、可口服的 SGLT2 抑制剂。
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