1318793-82-6Relevant articles and documents
PHENYL C-GLUCOSIDE DERIVATIVES, PREPARATION METHODS AND USES THEREOF
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Paragraph 0103, (2013/03/26)
The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof, wherein, the definitions of R5 and R6 are selected from the following: (1) R5=R6=Me; (2) R5=Me, R6=OMe; (3) R5=Me, R6=H; (4) R5=Me, R6=F; (5) R5=F, R6=H; and (6) R5=OMe, R6=H.
Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors
Zhao, Wen Jing,Shi, Yong Heng,Zhao, Gui Long,Wang, Yu Li,Shao, Hua,Da Tang, Li,Wang, Jian Wu
, p. 1215 - 1218 (2012/02/02)
A series of gem-dimethyl-bearing C-glucosides were designed and synthesized as SGLT2 inhibitors, with anhydrous aluminum chloride-mediated Friedel-Crafts alkylation to construct the gem-dimethyl functionality being the key step. The in vivo anti-hyperglycemic activity was evaluated with mice oral glucose tolerance test (OGTT), and all the synthesized compounds showed significant but less potent anti-hyperglycemic activity than the positive control dapagliflozin.
