C -Aryl glucoside SGLT2 inhibitors containing a biphenyl motif as potential anti-diabetic agents
Bioorganic & Medicinal Chemistry Letters(2015)
摘要
A series of highly active C-aryl glucoside SGLT2 inhibitors containing a biphenyl motif were designed and synthesized for biological evaluation. Among the compounds tested, compound 16l demonstrated high inhibitory activity against SGLT2 (IC50=1.9nM) with an excellent pharmacokinetic profile. Further study indicated that the in vivo efficacy of compound 16l was comparable to that of dapagliflozin, suggesting that further development would be worthwhile.
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关键词
SGLT2 inhibitor,Type 2 diabetes,C-Aryl glucoside,Biphenyl
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