中国果菜

为研发适配果菜绿色防控的新型抑菌药剂，本研究设计并合成了12个含硝基的芳香酰胺类化合物，通过核磁对结构进行了确证，并测试了目标化合物对4种常见病原菌的抑菌活性。结果表明，大部分化合物对番茄早疫病菌、油菜菌核病菌的抑菌活性较好，对黄瓜灰霉病菌和立枯丝核病菌的抑制活性较弱。构效关系研究表明，R²部分(氮原子相连苯环的取代基)引入6-甲基化合物抑菌活性影响较弱，R³部分(硝基取代苯环的取代基)引入硝基化合物抑菌活性普遍降低。发现化合物I-2(N-[3-[2,6-二硝基-4-(三氟甲基)苯氧基]苯基]-2-氟苯甲酰胺)、I-8(N-[3-[2,6-二硝基-4-(三氟甲基)苯氧基]苯基]-4-氟苯甲酰胺)和I-9(N-[3-[5-氯-2-硝基-4-(三氟甲基)苯氧基]苯基]-4-氟苯甲酰胺)具有较好的广谱活性，对四种病菌的抑制活性均在50%以上，化合物I-9活性最好，对油菜菌核病菌的抑菌活性为75.75%，可作为先导化合物进一步优化研究，为防治果菜重大病害提供解决方案，助力果菜产业绿色可持续发展。

To develop novel fungicides suitable for the green control of fruit and vegetable diseases, 12 nitro-containing aromatic amide compounds were designed and synthesized in this study. Their structures were confirmed by nuclear magnetic resonance(NMR), and their fungicidal activities against 4 common pathogenic fungi were evaluated. The results showed that most compounds exhibited moderate activity against Alternaria solani and Sclerotinia sclerotiorum, and weak activity against Botrytis cinerea and Rhizoctonia solani.Structure-activity relationship(SAR) analysis indicated that introduction of a 6-methyl group at the R² position had a weak effect on antifungal activity, whereas addition of a nitro group at the R³ position generally led to decreased activity. Compounds I-2, I-8 and I-9 displayed favorable broad-spectrum activity, with inhibitory rates exceeding 50% against four pathogens. Among them, compound I-9 showed the best activity, with inhibition rates of 75.75% against S. sclerotiorum, which could be used as a lead compound for further optimization, providing solutions for the control of major diseases in fruits and vegetables and contributing to the green and sustainable development of the fruit and vegetable industry.