1185339-63-2Relevant 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
, 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.
