α,β-不饱和羧酸苄酯的合成及其抑菌活性
Synthesis and Antifungal Activity of α,β-Unsaturated Benzyl Carboxylates
沙赟颖 1杨珊珊 1燕韦婷 1张卓周 1王立中 1翟子君 1刘竺云2
作者信息
- 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. 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;南京工业大学药学院,江苏 南京 211816
- 折叠
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.
Abstract
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Key words
α,β-unsaturated benzyl carboxylates/phytopathogenic fungi/antifungal activity/structure-activity relationship/benzyl ester引用本文复制引用
出版年
2024
国家科技期刊平台
NSTL
维普
万方数据