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番荔枝酰胺环状类似物的合成及抗氧化活性
引用本文:Xie P,Jiao XZ,Liang XT,Feng WH,Wei HL,Liu GT. 番荔枝酰胺环状类似物的合成及抗氧化活性[J]. 中国医学科学院学报, 2004, 26(4): 372-378
作者姓名:Xie P  Jiao XZ  Liang XT  Feng WH  Wei HL  Liu GT
作者单位:中国医学科学院,中国协和医科大学,药物研究所合成室,北京,100050
基金项目:国家重点基础研究发展计划(973计划)
摘    要:目的设计合成一系列番荔枝酰胺环状类似物并考察其抗氧化活性.方法以对羟基苯乙酸为原料,经9步反应,得到一系列3-位取代的吲哚-2-酮类化合物,其结构经核磁共振氢谱和质谱确定.结果11个3-位取代的吲哚-2-酮类化合物中化合物9和13的抗氧化活性和阳性对照FLZ-52活性相当.结论以番荔枝酰胺环状类似物FLZ-52为先导物进行的环合结构改造有一定效果,值得进一步研究.

关 键 词:番荔枝酰胺  吲哚-2-酮  合成  抗氧化活性
修稿时间:2004-03-17

Synthesis and antioxiactivity of squamosamide cyclic analogs
Xie Ping,Jiao Xiao-zhen,Liang Xiao-tian,Feng Wei-hong,Wei Huai-ling,Liu Geng-tao. Synthesis and antioxiactivity of squamosamide cyclic analogs[J]. Acta Academiae Medicinae Sinicae, 2004, 26(4): 372-378
Authors:Xie Ping  Jiao Xiao-zhen  Liang Xiao-tian  Feng Wei-hong  Wei Huai-ling  Liu Geng-tao
Affiliation:Department of Drug Synthesis, Institute of Materia Medica, CAMS and PUMC, Beijing 100050, China. pingxie123@vip.sohu.net
Abstract:Objective To design and synthesize a series of squamosamide cyclic analogues and to test their antioxidation activity. Methods Eleven 3-substituted indole-2-one derivatives were designed and synthesized through 9 steps with p-hydroxyphenylacetic acid as the starting material and their structures were confirmed by nuclear magnetic resonance and mass spectrometry. Results Eleven compounds showed antioxidation activity and the activities of compounds 9 and 13 matches the positive control FLZ-52. Conclusion Cyclic reconstruction with FLZ-52 as the lead compound have some antioxidation activity.
Keywords:squamosamide  indole-2-one  synthesis  antioxiactivity
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