Liu Yan, Zou Lan, Ma Lin, Chen Wen-Hua, Wang Bo, Xu Zun-Le
School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, PR China.
Bioorg Med Chem. 2006 Aug 15;14(16):5683-90. doi: 10.1016/j.bmc.2006.04.014. Epub 2006 May 2.
Considerable interest has been attracted in xanthone and its derivatives because of their large variety of pharmacological activities. In this project, a series of hydroxylxanthones and their acetoxy and alkoxy derivatives were synthesized and evaluated as alpha-glucosidase inhibitors, aimed at clarifying the structure-activity correlation. The results indicated that these xanthone derivatives were capable of inhibiting in vitro alpha-glucosidase with moderate to good activities. Among them, polyhydroxylxanthones exhibited the highest activities and thus may be exploitable as a lead compound for the development of potent alpha-glucosidase inhibitors.
氧杂蒽酮及其衍生物因其多种多样的药理活性而备受关注。在本项目中，合成了一系列羟基氧杂蒽酮及其乙酰氧基和烷氧基衍生物，并将其作为α-葡萄糖苷酶抑制剂进行评估，旨在阐明构效关系。结果表明，这些氧杂蒽酮衍生物能够在体外以中等至良好的活性抑制α-葡萄糖苷酶。其中，多羟基氧杂蒽酮表现出最高的活性，因此有望作为开发强效α-葡萄糖苷酶抑制剂的先导化合物。
