a School of Medicine and Life Sciences , University of Jinan-Shandong Academy of Medical Sciences , Jinan , Shandong , China.
b Institute of MateriaMedica , Shandong Academy of Medical Sciences , Jinan , Shandong , China.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):15-30. doi: 10.1080/14756366.2018.1518958.
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.
通过微波辐射加热合成了各种取代的 3-芳基香豆素衍生物。该方法具有环保、经济、简单分离和纯化过程、副产物少、反应收率高的特点。对这些 3-芳基香豆素衍生物进行了抗氧化、α-葡萄糖苷酶抑制和晚期糖基化终产物（AGEs）形成抑制活性筛选。大多数化合物表现出显著的抗氧化和 AGEs 形成抑制活性。抗糖尿病活性研究表明，化合物 11 和 17 在体内与标准药物格列本脲等效。根据实验结果，目标化合物 35 可作为开发新型抗糖尿病药物的先导化合物。整个实验表明，3-芳基香豆素具有抗糖尿病活性，为开发抗糖尿病活性药物增添了新的天然骨架。
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