杂环金属配合物的合成及抑菌活性

Synthesis of Five-membered Heterocycle-Copper(Ⅱ)Complexes and Antibacterial Activity

为寻找新型广谱的抗菌素先导化合物,以5-溴呋喃-2-羧酸和2-四氢糠酸为起始原料合成了2种五元杂环铜配合物,利用(1)^H NMR、(13)^C NMR对其结构及性质进行表征和分析,以平板菌落计数法测定铜配合物对大肠杆菌和金黄色葡萄球菌的抑制作用。初步体外抑菌活性显示,在0.038 mg/mL浓度下,目标化合物对两种细菌均具有较好的抑制活性。其中,5-(5-溴呋喃-2-基)-1,3,4-噻二唑铜(化合物4)的抑菌活性较强,其浓度与抑菌活性呈线性关系。

In order to find new broad-spectrum antibiotic lead compounds,two five-membered heterocycle-copper(Ⅱ)complexes was synthesized from 5-bromofuran-2-carboxylic acid and 2-tetrahydrofuroic acid,and their as starting materials,and their structures and properties were characterized and analyzed by(1)^H NMR and (13)^C NMR.The inhibitory effect of copper complexes on Staphylococcus aureus was determined by plate colony counting method.The preliminary in vitro antibacterial activity showed that the target compounds had good inhibitory activity against Staphylococcus aureus at the concentration of 0.038 mg/mL.Among them,5-(5-bromofuran-2-yl)-1,3,4-thiadiazole copper(compound 4)has stronger antibacterial activity,and its concentration has a linear relationship with the antibacterial activity.