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O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.

Bioorganic & medicinal chemistry letters (2009-08-25)
Baihua Xu, Binhua Lv, Yan Feng, Ge Xu, Jiyan Du, Ajith Welihinda, Zelin Sheng, Brian Seed, Yuanwei Chen
ABSTRACT

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.

MATERIALS
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Sigma-Aldrich
3-Bromo-4-methylbenzoic acid, technical grade, 85%