新型四氢异喹啉-C-芳基葡萄糖苷的合成及生物评价作为治疗 2 型糖尿病的 SGLT2 抑制剂。
Synthesis and biological evaluation of novel tetrahydroisoquinoline-C-aryl glucosides as SGLT2 inhibitors for the treatment of type 2 diabetes.
机构信息
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, PR China.
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, PR China.
出版信息
Eur J Med Chem. 2016 May 23;114:89-100. doi: 10.1016/j.ejmech.2016.02.053. Epub 2016 Mar 22.
A series of novel tetrahydroisoquinoline-C-aryl glucosides has been synthesized and evaluated for the inhibition of human SGLT2. Compared with dapagliflozin, compound 13h exhibited equivalent in vitro inhibitory activity against SGLT2, which might become a promising candidate for the treatment of type 2 diabetes.
一系列新型四氢异喹啉-C-芳基葡萄糖苷已被合成并评估其对人 SGLT2 的抑制作用。与达格列净相比，化合物 13h 对 SGLT2 的体外抑制活性相当，可能成为治疗 2 型糖尿病的有前途的候选药物。
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