一些噻二唑衍生物的合成及抑菌活性研究  

Synthesis and antibiosis activity of some compounds with thiadiazol structure

作　　者：袁海燕 董新[1] 黄燕敏[1] 展军颜 崔建国[1] 甘春芳[1] YUAN Hai-yan;DONG Xin;HUANG Yan-min;ZHAN Jun-yan;CUI Jian-guo;GAN Chun-fang(Guangxi Key Laboratory of Natural Polymer Chemistry and Physics,Key Laboratory of Beibu Gulf Environment Change and Resources Utilization,School of Chemistry and Materials,Nanning Normal University,Nanning 530001,China)

机构地区：[1]广西天然高分子化学与物理重点实验室北部湾环境演变与资源利用教育部重点实验室南宁师范大学化学与材料学院

出　　处：《化学研究与应用》2019年第6期1066-1072,共7页Chemical Research and Application

基　　金：广西高校科学技术研究项目(KY2015D077)资助;2018广西科技重大专项项目(2018AA22002)资助

摘　　要：以硫代氨基脲、甲酸、取代苯甲酸以硫代氨基脲、甲酸、取代苯甲酸为原料,通过脱水环化、Knoevenagle缩合反应等步骤,得到一类具有噻唑环和噻唑啉酮双杂环结构的化合物 6a^6h 。此外,将中间体4a^4h与三氯吡啶醇钠反应,得到另一类具有噻唑环和三氯吡啶醇结构的新型化合物7a^7g 。合成的终产物中,有9个化合物为新化合物。采用IR、NMR等方法对合成化合物进行了结构表征,并且利用生长速率法对目标产物的植物菌类抑菌活性进行测试,初步结果表明,部分化合物具有一定的抑菌活性,化合物6d对稻瘟病菌(Fusarium oxysporumf.sp.cubense)和番茄早疫病菌(Alternariasolani)具有良好的活性,在浓度为50 mg·L^-1 时,抑菌率达到80%以上。Using thiosemicarbazide,formic acid and substituted benzoic acid as starting materials,through dehydration and Knoevenagle reaction,a series of compounds containing both thiazole and thiazolinone with double heterocyclic structures were synthesized.In addition,another new type of compounds 7a^7g containing both thiazole and trichloropyridine double heterocyclic structures were synthesized.The structures of all the products were characterized by IR,NMR,and nine of them were new compounds.The antimicrobial activity of the target products was evaluated by the growth rate method.The results showed that some compounds displayed distinct inhibitory activity.Especially,compound 6d could effectively inhibit Fusarium oxysporumf.sp.cubense and Alternariasolani better than other compounds,and the inhibitory rate was above 80%at the concentration of 50 mg·L^-1 .

关 键 词：噻二唑 噻唑啉酮 三氯吡啶醇 杂环化合物 抑菌活性 

分 类 号：O626.25[理学—有机化学]