文档介绍：三、羟基苯甲酰腙类化合物体外抗菌活性研究
方法:采用琼脂二倍稀释法测定目标化合物对大肠杆菌、金黄色葡萄球菌、铜绿假单胞菌的最低抑菌浓度。结果:初步活性测试结果显示,该类化合物取代基的位置和性质可明显影响该类化合物抑菌活性。B 环上引入甲氧基和乙氧基会降低其抑菌活性,但若同时引入硝基,则使抑菌活性有所增强。结论:目标化合物具有一定的体外抑菌活性,苯环上取代基的类型和羟基数目可影响目标化合物的抗自由基活性。
关键词苯甲酰腙类化合物;DPPH•自由基;•OH 自由基;抑菌活性;构效关系
ABSTRACT
Background
In recent years, there has been a growing interest in substances which exhibit antioxidant and antimicrobial properties that can find application in clinical conditions. Acylhydrazones pounds characterized by the presence of a -CONHN=CH- group in their molecule. pounds have been extensively investigated for their biological activities, such as anticancer, anticonvulsant, anti-HIV, anti-inflammatory, antibacterial and antioxidant properties, have been associated with acylhydrazones, because of their versatile coordination chemistry characteristics and capability to generate varied molecular architecture and coordination geometry. In this study, we attempt to synthesize a series of hydroxyl substituted N'-benzoylhydrazone derivatives and have further tests on their antioxidant and antibacterial activities, hoping to discover the structure-activity relationships of hydroxyl substituted N'-benzoylhydrazone derivatives and find out some new structures with high anti-free radical and antibacterial activities.
Objective
To synthesis hydroxyl substituted benzoylhydrazide analogs, and to discuss the structure-relationship with scavenge free radicals and antibacterial activities.
Methods
① Synthesis
plexes were prepared by similar methods according to the reported procedure. Compounds 2 and 3 were prepared according to methods described in literature. The synthetic schema for the preparation of pounds starts with benzyl acid derivatives. Benzyl acid derivatives were allowed to react with ethanol to pound 2, which was made to react with an 80% hydrazine hydrate solution in ethanol to pound 3. Finally, the pounds 4a-q were obtained in good yields by pound 3 with corresponding aromatic aldehydes (Ar-CHO) in eth