2-芳基吲哚类化合物的合成及杀菌活性测定  

Synthesis and fungicidal activity determination of 2-aryl indole compounds

作　　者：高青青 李浩彤 霍静蕾 王彤萱 王凯 霍静倩[1] 张金林[1] GAO Qingqing;LI Haotong;HUO Jingei;WANG Tongxuan;WANG Kai;HUO Jingqian;ZhANG Jinin(College of Plant Protection,Hebei Agriculture University,Baoding 071000,China)

机构地区：[1]河北农业大学植物保护学院,河北保定071000

出　　处：《河北农业大学学报》2023年第5期83-88,110,共7页Journal of Hebei Agricultural University

基　　金：国家自然科学基金(31471786);河北省重点研发计划项目(22326512D).

摘　　要：本试验采用“一锅法”合成6个2-芳基吲哚类化合物,结构均经氢谱和高分辨质谱进行验证,采用菌丝生长速率法对目标化合物的离体杀菌活性进行评价。在100μg/mL浓度下化合物3a对立枯丝核菌的抑制率为80.3%;化合物3a和3f对禾谷丝核菌的抑制率为80%左右,优于阳性对照药剂三唑酮、氰烯菌酯和啶酰菌胺(P<0.05);化合物3a、3e和3f对黄瓜灰霉病的抑制率均在84%以上,与阳性对照相当。然后对化合物进行EC_(50)的测定,化合物3a对禾谷丝核菌EC_(50)为3.290μg/mL,优于对照药剂吡唑醚菌酯(P<0.05)。化合物3e和3f对黄瓜灰霉病EC_(50)值分别为7.408和9.662μg/mL,与阳性对照效果相当(P>0.05)。在100μg/mL浓度下评估了化合物3a、3e和3f对黄瓜灰霉病的活体防治效果,其中化合物3a防效达90%,与对照药剂啶酰菌胺和苯醚甲环唑效果相当(P>0.05)。本研究对新型杀菌活性化合物发现和新型杀菌作用靶标的挖掘具有重要意义。This paper adopted the“one pot method”to synthesize six 2-aryl indole compounds,and their structures were verified by hydrogen spectrum and high resolution mass spectrum.The fungicidal activities of the target compounds were evaluated by mycelium growth rate method.The inhibitory rate of compound 3a against Rhizoctonia solani at a concentration of 100μg/mL was 80.3%.The inhibitory rate of compounds 3a and 3e on R.cerealis was about 80%,which was better than the positive control agents Triadimefon(P<0.05),Phenamacril and Boscalid.The inhibitory rates of compounds 3a,3e and 3f on Botrytis cinerea were over 84%,which was equivalent to the positive control.The EC_(50) of the target compounds against the fungi was determined and the EC_(50) of compound 3a against R.cerealis was 3.290μg/mL,which was superior to the control drug pyraclostrobin(P<0.05).The EC_(50) values of compounds 3e and 3f against Botrytis cinerea were 7.408μg/mL and 9.662μg/mL,and the effect was equivalent compared with the control drug(P>0.05).The control effect of compound 3a,3e and 3f on Botrytis cinerea was evaluated in vivo conditions.The visual control effect of compound 3a was 90%at 100μg/mL,and the effect was equivalent compared with the control agents pyrimidazole and feniconazole(P>0.05).This study is of great significance to the discovery of new fungicidal active compounds and the exploration of new fungicidal targets.

关 键 词：2-芳基吲哚类化合物 设计合成 杀菌活性 

分 类 号：S482[农业科学—农药学]