芳香丙烯酸酯类蛇床子素衍生物的合成与抗菌活性

Synthesis and antibacterial activities of aromatic acrylate derivatives of Osthole

摘要:

在前期对蛇床子素研究的基础上,保留其优势结构,与芳香丙烯酸组合,设计合成了24个酯类衍生物,经₁^HNMR、₁₃^CNMR和元素分析对其进行结构确证。抗菌活性测试结果显示：化合物4h和4t的抗菌效果最为显著,前者对金黄色葡萄球菌(S. aureus)、耐甲氧西林金黄色葡萄球菌(MRSA)、大肠杆菌(E. coli)和耐氟喹诺酮大肠杆菌(FREC)的MIC分别为4、16、8和16 μg/mL,后者对S. aureus、MRSA、E. coli和FREC的MIC分别为2、8、4和8 μg/mL,对所测细菌的抑制活性优于前期化合物,具有潜在研究价值。关键词：芳香丙烯酸酯；蛇床子素衍生物；合成；抗菌活性中图分类号：R914.4；TQ465 文献标识码：A 文章编号：1003-5214 (2023) 08-0000-06

Abstract:

On the basis of previous research on osthole, twenty-four ester derivatives were designed and synthesized, and confirmed by ₁^H NMR, ₁₃^C NMR and elemental analysis. The result showed that the activities of compound 4h and 4t against S. aureus, MRSA, E. coli and FREC were the most significant, the MIC of 4h was 4, 16, 8, 16 μg/mL respectively, and the MIC of 4t was 2, 8, 4, 8 μg/mL respectively, and their inhibitory activities against the tested bacteria were better than that of previous compounds, which have potential research value.