取代苯基甲醛类脱氢枞酰腙化合物的合成及其体外抑菌活性研究  

Synthesis and in vitro Antibacterial Activity of Substituted Phenyl Formaldehyde Dehydroabietyl Hydrazone Compounds

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作  者:伍勇 黄春花 徐静 WU Yong;HUANG Chunhua;XU Jing(Department of Pharmacy,Sichuan Vocational College of Health and Rehabilitation,Zigong 643000,China)

机构地区:[1]四川卫生康复职业学院药学系,四川自贡643000

出  处:《化学与生物工程》2021年第2期36-39,共4页Chemistry & Bioengineering

基  金:自贡市重点科技计划项目(2018CZ30);四川卫生康复职业学院重点项目(CWKY-2018Z-03)。

摘  要:以脱氢枞酸为起始原料,经酰卤化、亲核取代、脱水缩合等3步反应合成了取代苯基甲醛类脱氢枞酰腙化合物(Ⅲa~Ⅲf),通过IR、1HNMR对其结构进行了表征,并采用琼脂二倍稀释法对其体外抑菌活性进行了评价。结果表明,目标化合物Ⅲa~Ⅲf的收率为53.1%~78.8%;6种目标化合物对金黄色葡萄球菌、粪肠球菌、肺炎链球菌、铜绿假单胞菌、大肠埃希菌、阴沟肠杆菌等6株菌株的抑菌活性均较弱,其中化合物Ⅲa、Ⅲc、Ⅲf的最低抑菌浓度均为128μg·mL^-1。该方法具有反应条件温和、操作简便、产物易分离等优点。Using dehydroabietic acid as a starting material,we synthesized substituted phenyl formaldehyde dehydroabietyl hydrazone compounds(Ⅲa-Ⅲf)by acylation and halogenation reaction,nucleophilic substitution reaction,and dehydration condensation reaction.Moreover,we characterized their structures by IR and 1HNMR,and evaluated the in vitro antibacterial activity by a two-fold agar dilution method.The results show that the yields of the target compoundsⅢa-Ⅲf are 53.1%-78.8%.The antibacterial activities of the six target compounds against Staphylococcus aureus,Enterococcus faecalis,Streptococcus pneumoniae,Pseudomonas aeruginosa,Escherichia coli,and Enterobacter cloacae are weak.The minimum inhibitory concentrations of the compoundsⅢa,Ⅲc,andⅢf are all 128μg·mL^-1.This method has the advantages of mild reaction conditions,simple operation,and easy separation of products.

关 键 词:脱氢枞酸 酰腙 合成 体外抑菌活性 

分 类 号:O626[理学—有机化学]

 

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