α,β-不饱和羧酸苄酯的合成及其抑菌活性  

Synthesis and Antifungal Activity ofα,β-Unsaturated Benzyl Carboxylates

作　　者：沙赟颖[1] 杨珊珊 燕韦婷 张卓周 王立中[1] 翟子君 刘竺云[1,2] SHA Yun-ying;YANG Shan-shan;YAN Wei-ting;ZHANG Zhuo-zhou;WANG Li-zhong;ZHAI Zi-jun;LIU Zhu-yun(School of Intelligent Pharmacy and New Chemical Materials,Taizhou Polytechnic College,Taizhou 225300,PRC;School of Pharmaceutical Sciences,Nanjing Tech University,Nanjing 211816,PRC)

机构地区：[1]泰州职业技术学院智能制药与化工新材料学院,江苏泰州225300 [2]南京工业大学药学院,江苏南京211816

出　　处：《湖南农业科学》2024年第12期72-76,共5页Hunan Agricultural Sciences

基　　金：2023年泰州市科技支撑计划(社会发展)项目(TS-202323);泰州市“凤城英才计划”青年科技人才托举工程(2023年度);2023年江苏高校“青蓝工程”优秀教学团队;2023年江苏省职业院校学生创新创业培育计划项目(G-2023-1730);2024年江苏高校“青蓝工程”优秀青年骨干教师(苏教师函[2024]14号)。

摘　　要：研究采用药效基团融合策略,设计合成了25个α,β-不饱和羧酸苄酯化合物,采用菌丝生长速率法测定了其对6种植物病原真菌的抑菌活性,并对抑菌活性较强的化合物进行了小麦幼苗安全性试验。结果表明:大多数化合物对供试真菌表现出较高的抑制率,化合物B9和B16对所有供试真菌的抑制率都大于80%,B2对5种供试真菌的抑制率大于80%。选取抑菌活性较强的化合物B9进行小麦幼苗安全性试验,发现B9对小麦幼苗的生长没有明显影响,总体表现出较高的安全性。构效分析表明,苯环上引入卤素原子有利于提高化合物的抑菌活性。Twenty-five unsaturated benzyl carboxylates were designed and synthesized according to the principle of active group splicing.The mycelial growth rate was determined to evaluate the inhibition rates of the compounds on 6 species of phytopathogenic fungi.Furthermore,the compound with the strongest antifungal activity was tested for the safe application in wheat seedlings.The results showed that most of the compounds had obvious inhibitory activity on the tested fungi.The inhibition rates of B9 and B16 on all tested fungi were more than 80%,and the inhibition rates of B2 on 5 species of tested fungi were more than 80%.Compound B9 showed no significant effect on the growth of wheat seedlings,demonstrating high safety.The structure-activity relationship analysis showed that the introduction of halogen atoms in the benzene ring was beneficial to improving the antifungal activity of the compounds.

关 键 词：α β-不饱和羧酸苄酯 植物病原真菌 抑菌活性 构效关系 苄酯 

分 类 号：O621.2[理学—有机化学]