新型含硫吡唑杂环的合成及其抗稻瘟病菌活性研究  

Synthesis and Bioactive Evalution of Novel Sulfur-containing Pyrazole Heterocycle Against Magnaporthe Grisea

作　　者：李明桦 董守诚 谢金鑫 邓志鹏 汤日元 LI Ming-hua;DONG Shou-cheng;XIE Jin-xin;DENG Zhi-peng;TANG Ri-yuan(College of Materials and Energy,South China Agriculture University,Guangzhou 510642,China)

机构地区：[1]华南农业大学材料与能源学院,广东广州510642

出　　处：《合成化学》2021年第10期837-843,共7页Chinese Journal of Synthetic Chemistry

基　　金：国家级大学生创新创业训练计划项目(201910564025)。

摘　　要：以吡唑为母体化合物,通过3条路径合成了吡唑二硫代氨基甲酸酯、吡唑硫代酰胺,以及氟虫腈中间体衍生物等共计14种含硫吡唑杂环化合物,其结构经^(1)H NMR,^(13)C NMR和MS(ESI)表征。采用生长速率法测试了化合物对稻瘟病菌(Magnaporthe Grisea)的抑菌活性。结果表明:在100 mg·L^(-1)浓度下,化合物2f,2i,3c有良好的抗稻瘟病菌活性,抑制率分别为81.9%、65.3%、63.6%。Pyrazole skeletons are used as the parent compound to synthesize pyrazole dithiocarbamates,pyrazole thioamides and derivatives of Fipronil intermediate through three reaction pathways.Fourteen sulfur-containing pyrazole heterocycles have been synthesized and their structures were characterized by ^(1)H NMR,^(13)C NMR and MS(ESI).The antifungal activities of these compounds against Magnaporthe grisea were tested by the growth rate method.The results showed that compounds 2f,2i and 3c had good antifungal activities against Magnaporthe grisea at the concentration of 100 mg·L^(-1),with inhibitory rates of 81.9%,65.3%and 63.6%,respectively.The results show that these pyrazole derivatives have potential for further development as inhibitors against Magnaporthe grisea.

关 键 词：含硫吡唑杂环 稻瘟病菌 生长速率法 合成 吡唑硫代酰胺 氟虫腈 

分 类 号：O626[理学—有机化学] O626.21[理学—化学]