Stereoselective synthesis of bioactive isosteviol derivatives as alpha-glucosidase inhibitors

作者：Wu Ya; Yang Jing Hua; Dai Gui Fu; Liu Cong Jun; Tian Guo Qiang; Ma Wen Yan; Tao Jing Chao^*

来源：Bioorganic & Medicinal Chemistry, 2009, 17(4): 1464-1473.

DOI：10.1016/j.bmc.2009.01.017

• Isosteviol
• 1,3-Diol
• Hydroxylation
• Beckmann fragmentation
• Indole
• alpha-Glycosidase

Considerable interest has been attracted in isosteviol and its derivatives because of their large variety of pharmacological activities. In this project, a series of novel compounds containing hydroxyl, hydroxymethyl group and heteroatom-containing frameworks fused with isosteviol structure were synthesized and evaluated as alpha-glucosidase inhibitors, aimed at clarifying the structure-activity correlation. The results indicated that these isosteviol derivatives were capable of inhibiting in vitro alpha-glucosidase with moderate to good activities. Among them, indole derivative 15b exhibited the highest activities and thus may be exploitable as a lead compound for the development of potent alpha-glucosidase inhibitors.

• 出版日期2009-2-15
• 单位郑州大学