1079083-50-3Relevant academic research and scientific papers
C-Aryl glucosides substituted at the 4′-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes
Xu, Baihua,Feng, Yan,Cheng, Huawei,Song, Yanli,Lv, Binhua,Wu, Yuelin,Wang, Congna,Li, Shengbin,Xu, Min,Du, Jiyan,Peng, Kun,Dong, Jiajia,Zhang, Wenbin,Zhang, Ting,Zhu, Liangcheng,Ding, Haifeng,Sheng, Zelin,Welihinda, Ajith,Roberge, Jacques Y.,Seed, Brian,Chen, Yuanwei
scheme or table, p. 4465 - 4470 (2011/09/12)
A series of C-aryl glucosides with various substituents at the 4′-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of alkyl or alkoxy substituents at the 4′-position was found to improve SGLT2 potency, whereas introduction of a hydrophilic group at this position was deleterious. Compounds with alkoxy-, cycloalkoxy- or cycloalkenyloxy-ethoxy scaffolds exhibited good inhibitory activity and high selectivity toward SGLT2. Selected compounds were investigated for in vivo efficacy.
Design and synthesis of fluorescent SGLT2 inhibitors
Lansdell, Mark I.,Burring, Denise J.,Hepworth, David,Strawbridge, Matthew,Graham, Emily,Guyot, Thierry,Betson, Mark S.,Hart, James D.
scheme or table, p. 4944 - 4947 (2009/05/07)
The design and synthesis of the first fluorophore-conjugated SGLT2 inhibitors is described. The mode of linking the fluorophore to the SGLT2 pharmacophore was found to be crucial in achieving optimum potency. Superior potency to phlorizin was provided by
