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吲哚-3-乙醛酰胺类化合物的合成及生物活性研究进展
引用本文:胡鸿雨,王飞,赵胜贤,方美娟. 吲哚-3-乙醛酰胺类化合物的合成及生物活性研究进展[J]. 合成化学, 2017, 25(2): 178-184. DOI: 10.15952/j.cnki.cjsc.1005-1511.2017.02.16207
作者姓名:胡鸿雨  王飞  赵胜贤  方美娟
作者单位:1. 浙江师范大学 行知学院,浙江 金华 321004;2. 厦门大学 药学院,福建 厦门 361102; 3. 浙江普洛得邦制药有限公司,浙江 东阳 322118
基金项目:国家自然科学基金资助项目
摘    要:综述了吲哚-3-乙醛酰胺类化合物(ID)的合成及生物活性的研究进展。ID具有抗肿瘤、抗病毒、抗菌、抗炎、腺苷受体功能调节、缓解疼痛和抗类风湿关节炎等多种生物活性,在药物化学领域有广泛应用。ID的合成方法主要为:吲哚母核与乙酰氯在乙醚(或THF)中于室温反应1 h制得含草酰氯结构的中间体;中间体与取代胺基化合物和二异丙基胺乙基胺反应合成ID。并对ID未来的应用作了简要展望。参考文献32篇

关 键 词:吲哚-3-乙醛酰胺  生物活性  合成  研究进展  综述  
收稿时间:2016-08-12

Research Progress on the Synthesis and Bioactivities of Indole-3-glyoxylamide Derivatives
HU Hong-yu,WANG Fei,ZHAO Sheng-xian,FANG Mei-juan. Research Progress on the Synthesis and Bioactivities of Indole-3-glyoxylamide Derivatives[J]. Chinese Journal of Synthetic Chemistry, 2017, 25(2): 178-184. DOI: 10.15952/j.cnki.cjsc.1005-1511.2017.02.16207
Authors:HU Hong-yu  WANG Fei  ZHAO Sheng-xian  FANG Mei-juan
Abstract:The synthesis and bioactivities of indole-3-glyoxylamide derivatives( ID) were reviewed with thirty two references. ID, which exhibited well bioactivities in antitumor, antivirus, antibacterial, anti-inflammatory, adenosine regulation, etc, were widely applied in pharmaceutical chemistry. The main method for synthesizing ID was as follows: the intermediate containing oxalyl chloride ( M ) was ob-tained by the reaction of indole nuclear parent with acetylchloride in diethyl ether( or THF) by reaction rt for 1h. ID were synthesized by the reaction of M with substituted amino compound and N,N-diiso-propylethylamine. The forecast of the application of ID was briefly proposed.
Keywords:indole-3-glyoxylamide  biological activity  synthesis  research progress  review
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