کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1257297 | 971554 | 2013 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design, synthesis and biological activity of cyclohexane-bearing C-glucoside derivatives as SGLT2 inhibitors Design, synthesis and biological activity of cyclohexane-bearing C-glucoside derivatives as SGLT2 inhibitors](/preview/png/1257297.png)
Seven cyclohexane-bearing C-glucoside derivatives (7, 9, 12, 13 and 17–19) were designed and synthesized as SGLT2 inhibitors starting from a potent SGLT2 inhibitor we discovered in earlier work, (1S)-1-deoxy-1-[4-methoxy-3-(trans-n-propylcyclohexyl)methylphenyl]-d-glucose (1). The in vitro and in vivo biological activities were evaluated by hSGLT2/hSGLT1 inhibition and urinary glucose excretion (UGE), respectively. Among the synthesized compounds 12, the 6-deoxy derivative of 1 was the most active and selective SGLT2 inhibitor (IC50 = 1.4 nmol/L against hSGLT2; selectivity = 1576). Compound 12 was a potent SGLT2 inhibitor, which could induce more urinary glucose than 1 and dapagliflozin in UGE.
Seven new SGLT2 inhibitors were designed and synthesized based on a potent SGLT2 inhibitor 1 discovered previously. In vitro and in vivo evaluations revealed that 6-deoxy derivative 12 was the most potent SGLT2 inhibitor and could induce more urinary glucose in UGE than parent compound 1 and even dapagliflozin.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 24, Issue 5, May 2013, Pages 429–432