3区 · 医学
Article
作者: Fujikura, Hideki ; Kamada, Noboru ; Hikawa, Hidemasa ; Shimizu, Kazuo ; Watanabe, Shinjiro ; Nishimura, Toshihiro ; Katsuno, Kenji ; Azumaya, Isao ; Arakawa, Koichi ; Fujimori, Yoshikazu ; Hiratochi, Masahiro ; Tatani, Kazuya ; Isaji, Masayuki ; Fushimi, Nobuhiko ; Nakabayashi, Takeshi
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.