5-去氢枞基-1,3,4-噁二唑-2-硫醇的微波合成及抗菌活性  

Microwave-assisted synthesis of 2-dehydroabietyl-1,3,4-oxadiazole 2-thiol and its antibacterial activity

作　　者：段文贵[1] 李行任[1] 莫启进[1] 苏建发[1] 罗德城[1] 黄丹平[1] 

机构地区：[1]广西大学化学化工学院,广西南宁530004

出　　处：《广西大学学报（自然科学版）》2009年第2期201-204,210,共5页Journal of Guangxi University（Natural Science Edition）

基　　金：广西林产化学品开发与应用重点实验室开放基金资助项目(GXFC08-04);广西研究生教育创新计划项目(2008105930703M088);广西大学"国家大学生创新性实验计划"校级项目

摘　　要：以去氢枞酸为原料,经酰化后与水合肼反应合成去氢枞酸酰肼.在微波辐照下,去氢枞酸酰肼与二硫化碳在碱性条件下环合制得5-去氢枞基-1,3,4-噁二唑-2-硫醇.通过元素分析、IR、MS、1H NMR和13C NMR对所合成化合物进行了结构表征.体外抗菌活性测试结果表明,该化合物对革兰氏阳性菌-金黄色葡萄球菌、革兰氏阴性菌-大肠杆菌和枯草杆菌均有较强的抗菌活性,其最低抑菌浓度(MIC)分别为4,8和4μg/mL.Dehydroabietic acid chloride was prepared by the reaction of dehydroabietic acid, the starting material, with thionyl chloride, followed by the reaction of the dehydroabietic acid chloride with excessive hydrazine hydrate to provide dehydroabietic acid hydrazide. Then, under microwave irradiation, the hydrazide was refluxed with carbon disulfide in the presence of potassium hydroxide to yield target compound 5-dehydroabietyl-1,3,4-oxadiazole-2-thiol. The target compound was characterized by IR, MS, 1HNMR, 13C NMR and elemental analysis. The biological tests showed that compound possessed obvious antibacterial activities against S. aureus, E. coli and B. subtili, at the minimal inhibitory concentration （MIC） of 4,8 and 4μg/mL, respectively.

关 键 词：去氢枞酸 1 3 4-噁二唑-2-硫醇 微波辅助合成 抗菌活性 

分 类 号：O626[理学—有机化学]