Author/Authors :
Baihua Xu، نويسنده , , Yan Feng، نويسنده , , Binhua Lv، نويسنده , , Yu-ge XU، نويسنده , , Lili Zhang، نويسنده , , Jiyan Du، نويسنده , , Shin-Kun Peng، نويسنده , , Min Xu، نويسنده , , Jiajia Dong، نويسنده , , Wenbin Zhang، نويسنده , , Ting Zhang، نويسنده , , Liangcheng Zhu، نويسنده , , Haifeng Ding، نويسنده , , Zelin Sheng، نويسنده , , Ajith Welihinda، نويسنده , , Brian Seed، نويسنده , , Yuanwei Chen، نويسنده ,
Abstract :
A series of 2-substituted C-aryl glucosides have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of an appropriate ortho substituent at the proximal phenyl ring adjacent to the glycosidic bond was found to improve SGLT2 inhibitory activity and dramatically increase selectivity for hSGLT2 over hSGLT1. Selected compounds were investigated for in vivo efficacy.
Keywords :
Diabetes , SGLT , Urinary glucose , ortho-Substituted C-aryl glucosides , Blood glucose , Sodium-dependent glucose co-transporter