Synthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agents

Journal of Enzyme Inhibition and Medicinal Chemistry

Jie Sun¹  Jie Yang¹  Teng Liu¹  Xiaojing Wang¹  Yuheng Hu¹  Bing Wang¹ 

[1] School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, Jinan, Shandong, China;Institute of MateriaMedica, Shandong Academy of Medical Sciences, Jinan, Shandong, China;Key Laboratory for Biotech-Drugs Ministry of Health, Jinan, Shandong, China;Key Laboratory for Rare & Uncommon Diseases of Shandong Province, Jinan, Shandong, Chin;

关键词: 3-Arylcoumarin;    α-glucosidase inhibitor;    antidiabetic;    AGEs inhibitor;   

DOI  :  10.1080/14756366.2018.1518958

来源: publisher

【 摘 要 】

A variety of substituted 3-arylcoumarin derivatives were synthesised through microwave radiation heating. The method has characteristics of environmental friendliness, economy, simple separation, and purification process, less by-products and high reaction yield. Those 3-arylcoumarin derivatives were screened for antioxidant, α-glucosidase inhibitory and advanced glycation end-products (AGEs) formation inhibitory. Most compounds exhibited significant antioxidant and AGEs formation inhibitory activities. Anti-diabetic activity studies showed that compounds 11 and 17 were equipotent to the standard drug glibenclamide in vivo. According to the experimental results, the target compound 35 can be used as a lead compound for the development of new anti-diabetic drugs. The whole experiment showed that anti-diabetic activity is prevalent in 3-arylcoumarins, which added a new natural skeleton to the development of anti-diabetic active drugs.

【 授权许可】

CC BY