樟脑酸基硫脲类化合物的合成及抑菌活性研究（英文）  

Synthesis and Antifungal Activity of Camphoric Acid-based Thiourea Derivatives

作　　者：马献力[1,2] 刘陆智[1] 段文贵[1] 石贤春 李芳耀[1,2] 华忠泽 

机构地区：[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

出　　处：《林产化学与工业》2015年第6期69-77,共9页Chemistry and Industry of Forest Products

基　　金：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)

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%)。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 werecharacterized 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-CH3 O） and camphoric acid-based （m-methoxy） phenyl thiourea 5d （ R = m-CH3 O） 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% ）.

关 键 词：樟脑酸 硫脲 合成 抑菌活性 

分 类 号：TQ35[化学工程]