周绪容,鄢伯钰,吴学姣,杨家强.化学通报,2022,85(11):1371-1375.
蛇床子素酯类/磺酸酯类衍生物的合成与抗菌活性研究
Synthesis and antibacterial activities of osthole ester/sulfonate derivatives
投稿时间:2022-01-29  修订日期:2022-03-30
DOI:
中文关键词:  蛇床子素  结构改造  酯类化合物  磺酸酯类化合物  合成  抗菌活性
英文关键词:Osthole, Structural modification, Ester derivatives, Sulfonate derivatives, Synthesis  Antibacterial activities
基金项目:贵州省卫生健康委科学技术基金项目(gzwkj2021-444)和遵义医科大学2018年度学术新苗培养及创新探索专项项目(黔科合平台人才[2018]5772-48)资助
作者单位E-mail
周绪容 遵义医科大学药学院 贵州 遵义 2630843926@qq.com 
鄢伯钰 遵义医科大学药学院 贵州 遵义  
吴学姣 遵义医科大学药学院 贵州 遵义  
杨家强 遵义医科大学药学院 贵州 遵义 yjqcn@126.com 
摘要点击次数: 90
全文下载次数: 0
中文摘要:
      为了寻找抗菌苗头化合物,以蛇床子素为原料,对其7位结构改造,经脱甲基化制得中间体Ⅰ,中间体Ⅰ再分别与酰氯、磺酰氯反应,合成了12个目标化合物,经1H NMR 、13C NMR和MS确认结构。体外抗菌活性筛选结果表明:两类衍生物对金葡菌有较好的抗菌活性,磺酸酯衍生物的活性优于羧酸酯衍生物,尤以化合物Ⅲd和Ⅲe的抗金葡菌的活性最为显著,MIC值均为32mg/L,远优于蛇床子素的活性,接近对照药苯唑西林。该研究也表明蛇床子素7位的结构修饰能改善其抗菌活性,值得进一步研究。
英文摘要:
      In order to find antibacterial hit compounds, the structural modification and antibacterial activities evaluation of osthole at C-7 side chain were carried out. Intermediate I was prepared from osthole by demethylation, then twelve target compounds were synthesized, and their structures were established by 1H NMR, 13C NMR and MS. The antibacterial activities of the products were evaluated by the agar dilution method. The results showed that the two derivatives had good inhibitory activities against S. aureus. And the activities of sulfonate derivatives were better than that of carboxylate derivatives, especially compounds Ⅲd and Ⅲe were the most significant, the MIC values against S. aureus were 32mg/L, which were much better than that of osthole and oxacillin. These studies also show that the structural modification of osthole at C-7 side chain can improve its antibacterial activities, which is worthy of further study.
查看全文  查看/发表评论  下载PDF阅读器
关闭