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含不饱和侧链异噻唑类抗菌剂的合成及其抗菌性能初步评价 被引量:8

Synthesis of isothiazoles antibacterial agent and evaluation of its property
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摘要 针对小分子有机抗菌剂存在耐热性差、基体相容性不好、渗出物安全性差等问题,设计合成用于高分子类抗菌剂的含有不饱和侧链的异噻唑类化合物。以3-巯基丙酸甲酯为原料,经氨解、关环、烯丙基化合成了2种含有不饱和侧链的异噻唑类化合物,分别为3-烯丙氧基异噻唑和N-烯丙基异噻唑啉酮。通过电子轰击质谱、核磁共振氢谱和碳谱对其产物及关键中间体的结构进行表征。2种含有不饱和侧链异噻唑类化合物的总收率达52%,优化后的合成路线条件温和,操作简单,易于控制。抗菌性能初步评价结果显示,2种异噻唑类化合物都具有良好的杀菌性能。 Due to the problems such as heat-resistance,compatibility and safety of exudates of small organic antibacterial compounds,two different isothiazole monomer with unsaturated side chain,i.e.3-allyloxyisothiazole and N-allylisothiazolone,were synthesized with 3-mercaptopropionate as the starting material through ammonolysis,cyclization and allylation reactions.All the resulted products and key intermediates were characterized with EI-MS,1H-NMR and13C-NMR.The combined overall yield of these two compounds was up to 52%.The optimized reaction process is mild,easy to manipulate and control.The results of antibacterial evaluation show that these two isothiazoles have good antibacterial property.
出处 《纺织学报》 EI CAS CSCD 北大核心 2009年第9期87-92,共6页 Journal of Textile Research
基金 北京市教委面上项目(KM200810012006)
关键词 合成 异噻唑啉酮 抗菌 表征 synthesis isothiazolone antibacterial characterization
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