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

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16 μg·mL^-1，后者对S.aureus、E.coli及MRSA的MIC分别为8、64和32 μg·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。

Abstract: 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 by ¹H NMR, ¹³C 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 16 μg·mL^-1, respectively, and the MIC of the Ⅱr was 8, 64 and 32 μg·mL^-1, respectively. The anti-MRSA activities of the two compounds is significant and is worthy of further structural optimization and study.