磷霉素壳寡糖盐的合成与抗菌活性测试

Synthesis and Antibacterial Activity of Fosfomycin Chitosan Oligosaccharide Salt

为了丰富磷霉素类药物的种类并获得更好的抗菌效果,采用拼合的方法合成了磷霉素壳寡糖盐。通过红外光谱、核磁共振氢谱对其结构初步地进行了结构表征,并采用滤纸片法验证和比较了磷霉素钙和磷霉素壳寡糖盐对大肠杆菌、金黄色葡萄球菌、肺炎克雷伯菌、铜绿假单胞菌的抑菌作用。以生物活性测试中抑菌圈的大小为评价指标,设计均匀实验,比较了左磷右胺盐与壳寡糖的质量比、反应温度、反应时间对磷霉素壳寡糖盐的抑菌活性的影响。确定了磷霉素壳寡糖盐的最佳制备条件是:左磷右胺盐与壳寡糖的质量比为1∶3,反应温度为25℃,反应时间为0.50 h。

To enrich the types of fosfomycin drugs and obtain better antibacterial activity,the fosfomycin chitosan oligosaccharide salt was synthesized by a splicing method.Its structure was initially characterized by infrared spectroscopy and 1H nuclear magnetic resonance spectroscopy.Its antibacterial activities towards escherichia coli,staphylococcus aureus,klebsiella pneumoniae and pseudomonas aeruginosa were further verified by the filter paper method and compared with that of fosfomycin calcium.Taking the size of inhibition zone in biological activity test as the evaluation index,we used uniform design of tests to compare the effects of the mass ratio of levophosphatidylamine salt and chitooligosaccharide,reaction temperature and reaction time on the antibacterial activity of fosfomycin chitosan oligosaccharide salt.The optimum preparation conditions are determined as follows:the mass ratio of levophosphoramine salt to chitosan oligosaccharide is 1∶3,the reaction temperature is 25℃ and the reaction time is 0.50 h.