Nie Wei, Luo Jian-Guang, Wang Xiao-Bing, Yin Hong, Sun Hong-Bin, Yao He-Quan, Kong Ling-Yi
Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, China.
Chem Pharm Bull (Tokyo). 2011;59(8):1051-6. doi: 10.1248/cpb.59.1051.
A series of α-glucosidase inhibitors with the oleanolic acid core and different cinnamic amide ligands were designed and synthesized. Their preliminary structure-activity relationships were analyzed. In general, the compounds with 3,28-disubstituted oleanolic acid exhibited stronger activity than those 28-monosubstituted analogues, and variation of cinnamic amide substitution significantly affected α-glucosidase inhibition activities. Most of the compounds showed potent inhibitory activity against α-glucosidase with much greater efficacy than a typical α-glucosidase inhibitor, acarbose.
设计并合成了一系列以齐墩果酸为核心、带有不同肉桂酰胺配体的α-葡萄糖苷酶抑制剂。分析了它们初步的构效关系。一般来说，具有3,28-二取代齐墩果酸的化合物比那些28-单取代类似物表现出更强的活性，并且肉桂酰胺取代基的变化显著影响α-葡萄糖苷酶抑制活性。大多数化合物对α-葡萄糖苷酶显示出强效抑制活性，其效果比典型的α-葡萄糖苷酶抑制剂阿卡波糖强得多。
