摘要
依据邻羟基二苯醚及酰肼类化合物的抗菌特性,以"邻羟苯基"为分子核心,构建了一类N-取代酰氯水杨酰肼类化合物.以水杨酸甲酯为原料,先经溴化反应制得5-溴水杨酸甲酯,再经肼解反应、最后与酰氯反应.抑菌测试表明,在质量浓度为0.01%时,目标化合物对对大肠杆菌的抑菌率均高于90.0%,具有较强抑菌活性;对白色念球菌和金黄色葡萄球菌具有一定的抑菌活性,表明该类化合物对不同菌株的抑菌活性具有一定的选择性和特异性;构效分析表明,邻羟基苯环上引入Br原子能够提高化合物的抑菌活性.
A series of N-（substituted chloride） salicylic hydrazide were designd by combining the molecule segment o-hydroxyphenyl according to antibacterial characteristics of o-hydroxydiphenyl ethers and hydrazide compounds.N-（substituted chloride）-salicylic hydrazide were synthesized by using methyl salicylate as raw material,through bromination,hydrazination and condensation reactions,respectively.The result of preliminary bioassay showed that the title compounds had about 90.0% inhibitory rate against Escherichia coli and had some inhibitory rate against Monilia albican and Staphylococcus aureus at 0.01% mass concentration.The analysis of structure activity show that the antibacterial activities were enhanced by the substituted halogen groups o-hydroxy ring.
出处
《天津理工大学学报》
2010年第4期4-6,共3页
Journal of Tianjin University of Technology
基金
国家自然科学基金(2057610320776114)
天津市自然科学基金(05YFJIYJC14000)
天津市高校科技发展基金(2006ZD3320050712)
关键词
N-取代酰氯水杨酰肼
水杨酸甲酯
合成
表征
抑菌活性
N-（substituted chloride）salicylic hydrazide
methyl salicylate
synthesis
characterization
antibacterial activity
