Xu Baihua, Lv Binhua, Feng Yan, Xu Ge, Du Jiyan, Welihinda Ajith, Sheng Zelin, Seed Brian, Chen Yuanwei
Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, Sichuan 610041, PR China.
Bioorg Med Chem Lett. 2009 Oct 1;19(19):5632-5. doi: 10.1016/j.bmcl.2009.08.030. Epub 2009 Aug 12.
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.
合成了两系列O-螺环C-芳基葡糖苷,并测试了它们对hSGLT1和hSGLT2的抑制作用。6'-O-螺环C-芳基葡糖苷在体外表现出强大的hSGLT2抑制活性,但在1微摩尔的筛选浓度下,2'-O-螺环C-芳基葡糖苷未显示出体外hSGLT2抑制活性。