蛇床子素酯类衍生物的合成及抗菌活性

Synthesis and Antibacterial Activities of Osthole Ester Derivatives

为了寻找抗菌活性化合物,以蛇床子素为原料,经氧化、还原、缩合反应制得12个蛇床子素酯类衍生物(Ⅲa-Ⅲl)。采用两倍稀释法测试目标化合物对金黄色葡萄球菌(S.aureus)、大肠埃希菌(E.coli)和耐甲氧西林金黄色葡萄球菌(MRSA)的体外抗菌活性。结果表明,该类衍生物呈现不同程度的抗菌活性,以化合物Ⅲi的活性最优,对S.aureus和MRSA的最小抑菌浓度(MIC)均为16 mg/L,远远优于蛇床子素的活性,尤其是抗MRSA活性较为显著,值得进一步结构优化和深入研究。

To find antibacterial compounds,a series of osthole ester derivatives was synthesized through three steps of oxidation,reduction,condensation reactions using osthole as the starting material.The antibacterial activities of these products were evaluated for S.aureus,E.coli and meticillin-resistant Staphylococcus aureus(MRSA)by the agar dilution method.The test results show that these derivatives have different degrees of antibacterial activities.Among them,compoundⅢi has the most significant antibacterial activities against S.aureus and MRSA and the minimum inhibitory concentration(MIC)values are 16 mg/L,and its anti-MRSA activity is more prominent.It is worthy of further structural optimization and study.