稠环磺酰胺衍生物的合成与抗菌活性研究  

Synthesis and antibacterial activities of novel sulfonamide derivatives containing a fused-ring

作　　者：杨家强 王越 周绪容 吴学姣 YANG Jia-qiang;WANG Yue;ZHOU Xu-rong;WU Xue-jiao(School of Pharmacy,Zunyi Medical University,Zunyi 563000,China)

机构地区：[1]遵义医科大学药学院,贵州遵义563000

出　　处：《药学学报》2021年第3期835-840,共6页Acta Pharmaceutica Sinica

基　　金：贵州省科技厅国际合作项目(黔科合外G字[2014]7013)。

摘　　要：为了寻找抗菌候选化合物,在前期研究基础上,18个稠环磺酰胺衍生物被设计合成,经1H NMR、13C NMR和MS确认结构。采用两倍稀释法对目标物进行体外抗菌活性测试,结果表明:该类衍生物对所测细菌有不同程度的抑制活性,尤以化合物Ⅱi、Ⅱr的抗菌活性最为突出,其中前者对金葡菌(S.aureus)、大肠埃希菌(E.coli)和耐甲氧西林金葡菌(MRSA)的最小抑菌浓度(MIC)分别为8、32和16μg·mL^(-1),后者对S.aureus、E.coli及MRSA的MIC分别为8、64和32μg·mL^(-1),两者的抗MRSA活性较显著,值得进一步结构优化和深入研究。To find antibacterial candidate compounds,eighteen novel sulfonamide derivatives containing a fused-ring were designed and synthesized on the basis of previous studies,with structures confirmed by1 H NMR,13 C NMR and MS.Antibacterial activities of the products were evaluated by the agar dilution method.The results show that these derivatives have different degrees of inhibitory activity on the tested bacteria,with the compounds IIi and IIr the most potent.The MIC of IIi for S.aureus,E.coli and MRSA was 8,32 and 16μg·mL^(-1),respectively,and the MIC of the IIr was 8,64 and 32μg·mL^(-1),respectively.The anti-MRSA activities of the two compounds is significant and is worthy of further structural optimization and study.

关 键 词：磺酰胺 稠环化合物 膦酸酯 合成 抗菌活性 

分 类 号：R916[医药卫生—药学]