摘要
为发现具有新颖结构的绿色杀菌剂,本研究以具有良好生物活性的天然产物香草醛为先导化合物,设计合成了30个未见文献报道的香草醛硫酸酯类衍生物,化合物结构均经过1H NMR、13C NMR和HRMS确证。通过菌丝生长速率法测定了目标化合物对水稻纹枯病菌(Rhizoctonia solani)、辣椒疫霉病菌(Phytophthora capsici)、苹果树腐烂病菌(Valsa mali)、苹果轮纹病菌(Botryosphaeria dothidea)、葡萄灰霉病菌(Botrytis cinerea)和小麦赤霉病菌(Fusarium graminearum)的抑制活性。结果表明:目标化合物在50μg/mL下对供试病原菌均表现出一定的抑制活性,其中化合物1s(O-(4-甲酰基-2-甲氧基)苯基-O'-(4-碘)苯基硫酸酯)、1u(O-(4-甲酰基-2-甲氧基)苯基-O'-(4-三氟甲基)苯基硫酸酯)和1x(O-(4-甲酰基-2-甲氧基)苯基-O'-(2-溴-4-氟)苯基硫酸酯)对苹果树腐烂病菌的EC50值分别为1.24、5.04和4.55μg/mL,表现出与对照药剂多菌灵相似的抑菌活性。化合物1s具有活性高、结构简单、易于合成等优点,可作为新型杀菌剂创制的先导化合物进一步开展结构优化研究。
In order to explore novel green fungicides,30 new vanillin sulfate derivatives were designed and synthesized using vanillin,a natural product with promising biological activity,as the lead compound.The structures of all compounds were confirmed by 1H NMR,13C NMR,and HRMS.The inhibitory effects of the target compounds against Rhizoctonia solani,Phytophthora capsici,Valsa mali,Botryosphaeria dothidea,Botrytis cinerea,and Fusarium graminearum were evaluated using the mycelial growth rate method.The results indicated that all target compounds exhibited inhibitory activities against the tested pathogens at a concentration of 50μg/mL.Notably,compounds 1s(O-(4-formyl-2-methoxy)phenyl-O'-(4-iodo)phenyl sulfate),1u(O-(4-formyl-2-methoxy)phenyl-O'-(4-trifluoromethyl)phenyl sulfate),and 1x(O-(4-formyl-2-methoxy)phenyl-O'-(2-bromo-4-fluoro)phenyl sulfate)showed significant activity against V.mali,with EC50 values of 1.24,5.04,and 4.55μg/mL,respectively.Their antifungal activity was comparable to that of the commercial control fungicide carbendazim.Compound 1s possesses advantages such as high activity,simple structure,and ease of synthesis,making it a promising lead compound for further structural optimization in the development of novel fungicides.
作者
王柯蒙
赵旺宇
张月瑶
李恒朝
胡兆农
WANG Kemeng;ZHAO Wangyu;ZHANG Yueyao;LI Hengzhao;HU Zhaonong(College of Plant Protection,Northwest A&F University,Yangling 712100,Shaanxi Province,China)
出处
《农药学学报》
北大核心
2026年第1期76-84,45,共10页
Chinese Journal of Pesticide Science
基金
国家自然科学基金(No.32502544,32372597)。
