【作者】 张学博； 雷鹏； 杨新玲； 徐高飞； 张小河； 凌云；

【Author】 ZHANG Xue-bo;LEI Peng;YANG Xin-ling;XU Gao-fei;ZHANG Xiao-he;LING Yun;Key Laboratory of Pesticide Chemistry and Application,Ministry of Agriculture,Department of Applied Chemistry,College of Science,China Agricultural University;

【机构】 中国农业大学理学院应用化学系农业部农药化学及应用重点开放实验室；

【摘要】 [目的]在前期工作基础上,通过活性亚结构拼接方法,设计了一系列取代苯甲醛缩氨基硫脲类化合物,以期发现有高活性化合物。[方法]经3步反应进行目标物的合成,并对所合成的目标化合物进行蘑菇酪氨酸酶活性测试及离体抑菌活性测试。[结果]合成了25个目标化合物,结构均经~1H NMR、IR、元素分析/高分辨质谱确证。[结论]酶活性测试结果表明,大多数化合物在50μg/mL对蘑菇酪氨酸酶表现出一定的抑制活性,离体抑菌活性测试结果表明,部分化合物对小麦全蚀病菌在50μg/mL浓度下的抑制率为100%,优于商品化对照药剂氟酰胺和氟吡菌胺。且化合物对蘑菇酪氨酸酶和小麦全蚀病菌抑制活性基本呈现出正相关的规律。推测该类化合物通过抑制酪氨酸酶的生物活性抑制小麦全蚀病菌的生长。更多还原

【Abstract】 [Aims]To find new compound with high biological activity,a series of substituted benzaldehyde thiosemicarbazone were designed with linking active sub-structures method.[Methods]The target compounds were synthesized in 4 steps and their anti-tyrosinase activity and fungicide biological effects were preliminarily evaluated.[Results]25 target compounds were obtained and their structures were confirmed by ~1H NMR spectra,IR spectrum,Elemental analysis or HRMS.[Conclusions]The tyrosinase results indicated that most target compounds exhibit certain inhibitory activity against mushroom tyrosinase under 50μg/mL concentration.Some compounds showed 100%inhibition against take-all pathogen of wheat,better than commercial agent flutolanil and fluopicolide under 50μg/mL concentration.Furthermore,the compounds showed positive correlation against tyrosinase and take-all pathogen of wheat.Speculated the compounds through inhibited tyrosinase bioactivity restrain the growth of take-all pathogen of wheat.更多还原