【作者】 王闽龙； 杜颖； 刘春辉； 杨新玲； 纪明山； 李兴海；

【Author】 WANG Minlong;DU Ying;LIU Chunhui;YANG Xinling;JI Mingshan;LI Xinghai;College of Plant Protection, Shenyang Agricultural University;College of Science,China Agricultural University;

【机构】 沈阳农业大学植物保护学院； 中国农业大学理学院；

【摘要】 [目的]为了获得具有高效杀菌活性的化合物,探索合成了结构新颖的2-烷基酰胺基-2-取代苯基乙磺酰胺类化合物。[方法]以N-（2-三氟甲基-4-氯苯基）-2-（3,5-二氟苯基）-2-氧代乙磺酰胺为先导,经还原胺化,与烷基酰氯对接获得目标产物,测试其对灰葡萄孢的离体和活体杀菌活性,并利用3D-QSAR模型进行构效关系分析。[结果]合成了23个结构新颖的2-烷基酰胺基-2-取代苯基乙磺酰胺,确证其构效关系,发现了高活性化合物V-17(EC₅₀值为0.66μg/mL)。[结论]该类化合物具有很好的杀菌效果,有进一步开发的价值。更多还原

【Abstract】 [Objective]To explore the novel structure compounds with high fungicidal activity,a series of novel 2-substituted alkyl-2-substituted phenyl ethylsulfonamides were synthesized.[methods]The title compounds were synthesized from the lead compound N-（2-trifluoromethyl-4-chlorophenyl）-2-（3,5-difluorophenyl）-2-oxo ethylsulfonamides by reductive amination and aryl chloride reaction.Their fungicidal activities in vitro and in vivo were also tested against Botrytis cinerea,and a three-dimensional quantitative structure-activity relationship（3 D-QSAR）model was developed to identify some key structural features responsible for their potency.[result]A total of 23 2-substituted alkyl-2-substituted phenyl ethylsulfonamides were synthesized.The QSAR of title compounds were also analyzed,and the compound V-17 showed excellent activity with the EC₅₀ value of 0.66 μg/mL against B.cinerea.[Conclusion]These compounds show good fungicidal activities and can be used as possible new lead compounds for further developing novel fungicides against B.cinerea.更多还原