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N-杂环苯甲酰芳胺衍生物的构效关系研究导致了一种对 var. 和四种小麦病原菌具有高度杀菌活性的候选药物。

Structure-Activity Studies of N-Heterocyclic Benzoyl Arylamine Derivatives Led to a Highly Fungicidal Candidate against var. and Four Wheat Pathogens.

机构信息

Plant Protection College of Henan Agricultural University, Zhengzhou 450002, People's Republic of China.

出版信息

J Agric Food Chem. 2022 Aug 24;70(33):10305-10315. doi: 10.1021/acs.jafc.2c03455. Epub 2022 Aug 11.

DOI:10.1021/acs.jafc.2c03455
PMID:35950372
Abstract

Wheat root diseases can seriously reduce yields and quality of wheat. 1,2,4-Triazole benzoyl arylamine derivatives previously showed good activities against some wheat root fungal pathogens. To further systematically disclose the structure-activity relationship, a series of benzoyl arylamines were designed and prepared. Their structures were characterized and fungicidal activities against var. and were evaluated. The results indicated that the structure of the N-heterocyclic group and the substituted group and their position on the benzamide scaffold had an important influence on the activities, as predicted. Finally, compound was found to show excellent activities against var. , , , , and with half-maximum effective concentrations of 0.002, 0.093, 0.011, 0.881, and 0.287 μg/mL, respectively. These results proposed that compound deserved serious consideration as a novel fungicide candidate for the control of wheat root diseases.

摘要

小麦根病可严重降低小麦的产量和品质。1,2,4-三唑苯甲酰芳胺衍生物先前表现出对一些小麦根真菌病原体的良好活性。为了进一步系统地揭示构效关系,设计并制备了一系列苯甲酰芳胺。对其结构进行了表征,并评价了它们对 和 的杀菌活性。结果表明,N-杂环基团和取代基的结构及其在苯甲酰胺支架上的位置对活性有重要影响,这与预测结果一致。最后,化合物 对 、 、 、 和 表现出优异的活性,其对 的半数有效浓度(EC50)分别为 0.002、0.093、0.011、0.881 和 0.287μg/mL。这些结果表明,化合物 值得作为一种新型杀菌剂候选物,以控制小麦根病。

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