title: Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2.
abstract: In order to investigate SAR regarding glucose moiety in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on glucose was conducted to explore potential utility as a suitable replacement of glucose per se. Among the compounds prepared, deshydroxy 29 (IC(50)=7.01nM) demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date. But, none of the compounds were better than the parent molecule 5 (IC(50)=1.75nM).
authors.affiliation: Green Cross Corporation, Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
authors.forename: Eun-Jung
authors.initials: EJ
authors.lastname: Park
authors.forename: Younggyu
authors.initials: Y
authors.lastname: Kong
authors.forename: Jun Sung
authors.initials: JS
authors.lastname: Lee
authors.forename: Sung-Han
authors.initials: SH
authors.lastname: Lee
authors.forename: Jinhwa
authors.initials: J
authors.lastname: Lee
mesh_terms: D003920:Diabetes Mellitus / Q000188:drug therapy* / Q000201:enzymology; D006027:Glycosides / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology*; D051297:Sodium-Glucose Transporter 2 / Q000378:metabolism*; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology
chemical_list: D006027:Glycosides; D007004:Hypoglycemic Agents; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013844:Thiazoles