Discovery of remogliflozin etabonate: A potent and highly selective SGLT2 inhibitor

[Display omitted] 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 poten...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2021-03, Vol.34, p.116033-116033, Article 116033
Hauptverfasser:	Shimizu, Kazuo, Fujikura, Hideki, Fushimi, Nobuhiko, Nishimura, Toshihiro, Tatani, Kazuya, Katsuno, Kenji, Fujimori, Yoshikazu, Watanabe, Shinjiro, Hiratochi, Masahiro, Nakabayashi, Takeshi, Kamada, Noboru, Arakawa, Koichi, Hikawa, Hidemasa, Azumaya, Isao, Isaji, Masayuki
Format:	Artikel
Sprache:	eng
Schlagworte:	Biochemistry & Molecular Biology Chemistry Chemistry, Medicinal Chemistry, Organic Life Sciences & Biomedicine O-glucoside Pharmacology & Pharmacy Physical Sciences Remogliflozin etabonate Science & Technology SGLT2 inhibitor Type 2 diabetes mellitus
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Zusammenfassung:	[Display omitted] 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.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2021.116033