含1,3,4-噻二唑硫醚的吡唑酰胺类化合物合成及生物活性  

Synthesis and Biological Activity of Novel Pyrazole Amide Derivatives Containing 1,3,4-Thiadiazole Thioether Moiety

作　　者：谢艳[1] 龚华玉[1] 王晓斌[1] 阮祥辉 张菊平[1] 李琴[1] 肖维[1] 薛伟[1] 

机构地区：[1]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,教育部绿色农药与生物工程重点实验室,贵阳550025

出　　处：《农药》2016年第12期872-876,共5页Agrochemicals

基　　金：国家自然科学基金资助项目(21462012);贵州省优秀青年科技人才项目(201535);贵州大学研究生创新基金资助项目(2016076)

摘　　要：[目的]寻找具有较好生物活性的活性分子。[方法]在吡唑酰胺的骨架中引入具有良好生物活性的1,3,4-噻二唑硫醚结构,设计合成一系列结构中含1,3,4-噻二唑硫醚的吡唑酰胺类化合物,并进行目标化合物的抗病毒和抑菌活性测试。[结果]所合成目标化合物结构经IR、1H NMR、13C NMR和元素分析确证。生物活性测试结果表明:在50 mg/L的浓度下,化合物对小麦赤霉病菌、苹果腐烂病菌和辣椒枯萎病菌有一定的抑制作用,但相对较差,同时,在500 mg/L的质量浓度下,部分目标化合物具有较好的抗烟草花叶病毒(TMV)活性。[结论]含1,3,4-噻二唑硫醚结构的吡唑酰胺类化合物对烟草花叶病毒(TMV)有较好的抑制活性,在其结构基础上进行进一步的结构修饰,有望得到具有较高抗病毒活性的有机活性分子。[Aims] This paper aims to explore active molecules with potent biological activities. [Methods] A series of pyrazole amide derivatives containing 1,3,4-thiadiazole thioether moiety were synthesized via the method of combing the 1,3,4-thiadiazole thioether group into the structure of pyrazole amides, and their antiviral activities and antifungal activities were evaluated. [Results] The title compounds were confirmed by IR, ^1H NMR, ^13C NMR and elemental analysis, and the results of biological assay indicated that most of compounds shown good antiviral activities against tobacco mosaic virus （TMV） at 500 mg/L and inferior antifungal activities against Fusarium oxysporum, Cytospora mandshurica, and Gibberella zeae at 50 mg/L. [Conclusions] The pyrazole amide derivatives containing 1,3,4-thiadiazole thioether moiety exhibited good antiviral activities against tobacco mosaic virus （TMV） and some small organic molecules with potent biological activities might be obtained via the structural modification based on the pyrazole amide derivatives bearing 1,3,4-thiadiazole thioether moiety.

关 键 词：吡唑酰胺 1 3 4-噻二唑硫醚 抗病毒活性 抑菌活性 

分 类 号：O626[理学—有机化学]