O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Two series of O-spiro C-aryl glucosides were synthesized and tested for inhibition of hSGLT1 and hSGLT2. 6'-O-Spiro C-aryl glucosides exhibited potent in vitro hSGLT2 inhibitory activity but 2'-O-spiro C-aryl glucosides showed no in vitro hSGLT2 inhibitory activity at a screening concentration of 1microM.
Xu
Baihua
B
Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, Sichuan 610041, PR China. xubaihua2002@163.com
Lv
Binhua
B
Feng
Yan
Y
Xu
Ge
G
Du
Jiyan
J
Welihinda
Ajith
A
Sheng
Zelin
Z
Seed
Brian
B
Chen
Yuanwei
Y
D005947:Glucose / Q000378:metabolism; D005960:Glucosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D051269:Sodium-Glucose Transporter 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D051297:Sodium-Glucose Transporter 2 / Q000378:metabolism; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D005960:Glucosides; D051269:Sodium-Glucose Transporter 1; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013141:Spiro Compounds; D005947:Glucose