| 2-氰基-3-(4-甲基苯并[d]噻唑-2-氨基)-3-苯基丙烯酸酯类化合物的合成及抗病毒活性 |
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| 引用本文： | 李娜,魏学,范会涛,毕亮,李向阳,杨松,胡德禹,宋宝安.2-氰基-3-(4-甲基苯并[d]噻唑-2-氨基)-3-苯基丙烯酸酯类化合物的合成及抗病毒活性[J].有机化学,2011,31(8). |
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| 作者姓名： | 李娜 魏学 范会涛 毕亮 李向阳 杨松 胡德禹 宋宝安 |
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| 作者单位： | 贵州大学精细化工研究开发中心 绿色农药与农业生物工程国家重点实验室培育基地/教育部重点实验室 贵阳550025 |
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| 基金项目： | 国家重点基础研究发展计划(“973”计划)(No.2010CB126105); 国家“973”计划前期(No.2010CB134504); 国家自然科学基金(No.20872021)资助项目 |
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| 摘 要： | 以氰乙酸乙酯(氰乙酸)为起始原料,经酯化、缩合、氯化,然后与2-氨基-4-甲基苯并d]噻唑反应,合成了20个新化合物4.所有化合物结构经过IR,1H NMR,13C NMR和元素分析确证.初步生物活性测试表明:在500μg·mL-1浓度下,该类化合物4具有一定的抗黄瓜花叶病毒(CMV)及抗烟草花叶病毒(TMV)室内活体治疗活性,其中化合物4b,4o,4q对CMV具有较好的活体治疗活性(抑制率分别为45.81%,43.20%,43.09%),化合物4d,4f,4h,4l对TMV具有较好的活体治疗活性(抑制率分别为45.68%,45.19%,45.86%,44.32%),对照药宁南霉素的活体治疗活性分别为56.31%,54.63%.
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| 关 键 词： | 2-氰基-3-苯基丙烯酸酯 2-氨基-4-甲基苯并[d]噻唑 合成 抗病毒活性 |
Synthesis and Antiviral Activity of 2-Cyano-3-(4-methyl-benzo[d]thiazol-2-amino)-3-phenyl Acrylate Derivatives |
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| Li Na,Wei Xue,Fan Huitao,Bi Liang,Li Xiangyang,Yang Song,Hu Deyu,Song Baoan.Synthesis and Antiviral Activity of 2-Cyano-3-(4-methyl-benzo[d]thiazol-2-amino)-3-phenyl Acrylate Derivatives[J].Chinese Journal of Organic Chemistry,2011,31(8). |
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| Authors: | Li Na Wei Xue Fan Huitao Bi Liang Li Xiangyang Yang Song Hu Deyu Song Baoan |
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| Institution: | Li,Na Wei,Xue Fan,Huitao Bi,Liang Li,Xiangyang Yang,Song Hu,Deyu Song,Baoan*(State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering,Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Research and Development Center for Fine Chemicals,Guizhou University,Guiyang 550025) |
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| Abstract: | In order to explore novel cyanoacrylates with highly antiviral activity,twenty new compounds 4 were synthesized by using ethyl cyanoacetate(cyanoacetic acid) as starting material,in four steps reaction including esterification,condensation,chlorination,and reaction with 2-amino-4-methylbenzod]thiazole.All synthesized new compounds were confirmed by IR,1H NMR,13C NMR spectra and elemental analysis.The preliminary bioassay revealed that title compounds possessed moderate to anti-CMV,anti-TMV activities at 50... |
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| Keywords: | 2-cyano-3-phenylacrylate 2-amino-4-methylbenzo[d]thiazole synthesis antiviral activity |
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