含氨基噻唑肟结构的膦酸酯衍生物的合成与抗菌活性研究

Synthesis and antibacterial activities of phosphonate derivativescontaining aminothiazoloxime fragment

采用分子杂合原理,将氨基噻唑肟与膦酸酯片段组合,设计合成了15个目标物进行抗菌活性研究。结果显示:该类衍生物对所测试细菌有较好的抑制作用,尤以化合物Ⅲf和Ⅲi的抗金葡菌(S.aureus)、大肠杆菌(E.coli)、耐甲氧西林金葡菌(MRSA)和耐氟喹诺酮大肠杆菌(FREC)活性最为显著,前者的最小抑菌浓度(MIC)分别为1、8、4和16μg·mL^(-1),后者的MIC分别为4、4、16和8μg·mL^(-1),抗S.aureus活性略低于苯唑西林,抗E.coli、MRSA和FREC活性优于对照药苯唑西林,值得进一步深入研究。

Based on the principle of molecular hybridization,fifteen compounds were designed and synthesized through the combination of aminothiazoloxime and phosphonate fragment.The results showed that these compounds had better inhibitory effects on the tested bacteria.In particular,the activities of compoundsⅢf andⅢi against S.aureus,E.coli,methicillin-resistant S.aureus(MRSA)and fluoroquinolone-resistant E.coli(FREC)were the most significant,the minimal inhibitory concentration(MIC)ofⅢf was 1,8,4,16μg·mL^(-1)respectively,and the MIC ofⅢi was 4,4,16,8μg·mL^(-1)respectively,which were slightly lower than that of the control drug oxacillin,and their anti-E.coli,MRSA and FREC activities were superior to that of the control drug oxacillin.Their activities to S.aureus were close to that of oxacillin,and to E.coli,MRSA and FREC were superior to that of oxacillin,which is worthy of further study.