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林产化学与工业 ›› 2015, Vol. 35 ›› Issue (6): 69-77.doi: 10.3969/j.issn.0253-2417.2015.06.012

• 研究报告 • 上一篇    下一篇

樟脑酸基硫脲类化合物的合成及抑菌活性研究

马献力1,2, 刘陆智1, 段文贵1, 石贤春1, 李芳耀1,2, 华忠泽1   

  1. 1.广西大学 化学化工学院, 广西 南宁 530004;
    2.桂林医学院 药学院, 广西 桂林 541004
  • 收稿日期:2014-12-08 出版日期:2015-12-25 发布日期:2015-12-28
  • 通讯作者: 段文贵(1964—),广西资源人,教授,博士生导师,主要从事天然资源化学和有机合成研究;E-mail:wgduan@gxu.edu.cn E-mail:wgduan@gxu.edu.cn
  • 作者简介:马献力(1978—),男,河南叶县人,博士生,从事天然产物改性及有机合成研究
  • 基金资助:
    国家自然科学基金资助项目(31260164);广西高校科学技术研究重点项目(ZD2014098)

Synthesis and Antifungal Activity of CamphoricAcid-based Thiourea Derivatives

MA Xian-li1,2, LIU Lu-zhi1, DUAN Wen-gui1, SHI Xian-chun1, LI Fang-yao1,2, HUA Zhong-ze1   

  1. 1. School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China;
    2. School of Pharmacy, Guilin Medical University, Guilin 541004, China
  • Received:2014-12-08 Online:2015-12-25 Published:2015-12-28

摘要: 以樟脑酸和氨乙基取代苯基硫脲为原料,合成了10个新型的樟脑酸基硫脲类化合物(5a-5j)。利用FT-IR、1H NMR、13C NMR、LC-MS和元素分析等手段对目标产物进行了结构表征。同时对化合物5a-5j的抑菌活性进行了测试。初步的生物活性测试表明,在质量浓度为50 mg/L时,大部分化合物具有一定的抑菌活性,其中化合物樟脑酸基邻甲氧基苯基硫脲5c(R=o-CH3O)和樟脑酸基间甲氧基苯基硫脲5d(R=m-CH3O)对番茄早疫病菌(Alternaria solani)的抑制率达86.9 %,化合物樟脑酸基间甲氧基苯基硫脲5d、樟脑酸基间甲基苯基硫脲5g(R=m-CH3)和樟脑酸基对溴苯基硫脲5i(R=p-Br)对苹果轮纹病菌(Physalospora piricola)的抑制率达86.1 %。此外,化合物5i还对花生褐斑病毒(Cercospora arachidicola)具有最好的抑制率(73.6%)。

关键词: 樟脑酸, 硫脲, 合成, 抑菌活性

Abstract: Ten novel camphoric acid-based thiourea compounds (5a-5j) were prepared using camphoric acid and aminoethyl substituted phenyl thioureas as starting materials.The target compounds were characterized by FT-IR, 1H NMR, 13C NMR, LC-MS, and elemental analysis.The antifungal activities of the compounds 5a-5j were tested.The preliminary bioassay showed that most of the target compounds exhibited certain antifungal activities, in which camphoric acid-based (o-methoxy)phenyl thiourea 5c (R=o-CH3O) and camphoric acid-based (m-methoxy)phenyl thiourea 5d (R=m-CH3O) had inhibition rate of 86.9 % against Alternaria solani, and camphoric acid-based (m-methoxy)phenyl thiourea 5d, camphoric acid-based (m-methyl)phenyl thiourea 5g (R=m-CH3) and camphoric acid-based (p-bromo)phenyl thiourea 4i (R=p-Br) had inhibition rate of 86.1 % against Physalospora piricola at the concentration of 50 mg/L.In addition, compound 5i also had the best inhibitory activity against cercospora arachidicola(73.6%).

Key words: camphoric acid, thiourea, synthesis, antifungal activity

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