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

Authors :
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
Source :
Bioorganic & Medicinal Chemistry. Mar2021, Vol. 34, pN.PAG-N.PAG. 1p.
Publication Year :
2021

Abstract

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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
09680896
Volume :
34
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
148806763
Full Text :
https://doi.org/10.1016/j.bmc.2021.116033