阿散酸-TMP的制备与体外抗菌活性研究

以阿散酸和甲氧苄啶(TMP)为原料,制备阿散酸-TMP,采用IR、熔点对其进行了表征;正交试验确定了最优反应条件为:反应温度80 ℃,反应时间3 h,反应物料比1.1∶1(阿散酸∶TMP)。通过体外抑菌试验来测试其抑菌效果,结果表明,阿散酸-TMP对5种供试菌的抑菌圈直径都在20 mm以上,显著大于阿散酸与TMP的混合物(P＜0.05);阿散酸-TMP对埃希氏大肠杆菌、金黄色葡萄球菌、鸡白痢沙门氏菌、福氏志贺氏菌、藤黄微球菌的MIC分别为32、64、256、32、128 μg/mL,均小于阿散酸与TMP的混合物。阿散酸-TMP对供试菌的抑菌效果好于阿散酸、TMP及阿散酸与TMP的混合物。

Preparation of Arsanilic Acid-TMP and its in vitro Antibacterial Activity

Arsanilic acid and TMP were utilized as the raw materials and then arsanilic acid-TMP was prepared.The new compound was characterized by IR and melting point.Orthogonal test showed that the best reaction condition was that being heated at 80 ℃ for 3 hours under reflux,and the molar ratio of arsanilic acid and TMP was 1.1∶1.The in vitro antibacterial indicated that the inhibitory zone diameter of arsanilic acid-TMP against the five kinds of tested bacteria is longer than 20 mm and arsanilic acid-TMP had greater bacteria-inhibiting effect than the physical mixture of arsanilic acid and TMP(P<0.05);the minimum inhibitory concentration(MIC) of arsanilic acid-TMP against Escherichia coli,Staphylococus aureus,Salmonella pullorum,Shigella flexneri and Micrococcus luteus were 32,64,256,32,128 μg/mL,respectively,which were less than the MIC of the physical mixture of arsanilic acid and TMP.According to this study,arsanilic acid-TMP has greater antibacterial effect than arsanilic acid,TMP and their physical mixture.