【作者】 张晓鸣； 雷鹏； 苏惠飞； 杨新玲； 张学博； 孙腾达； 马航宇； 凌云；

【Author】 ZHANG Xiao-ming;LEI Peng;SU Hui-fei;YANG Xin-ling;ZHANG Xue-bo;SUN Teng-da;MA Hang-yu;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]本文以天然产物Aspernigerin为先导,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（E）-3-苯基-1-（4-（1,2,3,4-四氢喹啉-1-硫羰基）哌嗪-1-基）丙-2-烯-1-酮类类化合物,以期发现有高活性的先导化合物。[方法]以1,2,3,4-四氢喹啉为起始原料,经5步反应进行目标物的合成,并进行了初步生物活性评价。[结果]合成了14个目标化合物,结构均经¹HNMR,HRMS分析确证。[结论]生测结果表明,部分目标化合物具有一定的离体杀菌活性,其中化合物7b对苹果腐烂病菌的抑制活性(EC₅₀=3.04μg/mL)优于对照药剂氟酰胺(EC₅₀=9.16μg/mL),可作为二级先导进行进一步的优化研究。更多还原

【Abstract】 [Aims]Based on the preliminary work and choosing the natural product Aspernigerin as the lead compound,a series of（E）-3-phenyl-1-（4-（1,2,3,4-tetrahydronaphthalene-l-carbonothioyl）piperazin-1-yl）prop-2-en-1-one with linking active sub-structures method to find new lead compound with high biological activity.[Methods]The target compounds were synthesized from substituted benzoic acid in 5 steps and their biological effects were preliminarily evaluated.[Results]14 target compounds were obtained and their structures were confirmed by ¹ H NMR spectra and HRMS.[Conclusions]The in vitro bioassay results indicated that some target compounds exhibit certain fungicidal activity.The bioassay results indicated that 5 b exhibited good anti-fungual activity against Valsa mali(EC₅₀ = 3.04μg/mL),which was better than the commercial fungicide fluoramide(EC₅₀= 9.16 μg/mL).更多还原