新型蛇床子素磺酸酯衍生物的合成与抗菌活性研究

目的 为了寻找抗菌候选化合物,对天然产物蛇床子素蛇床子素进行结构改造和生物活性评价.方法 以蛇床子素为原料,经二氧化硒氧化制得中间体1,中间体1经硼氢化钠还原制得中间体2,中间体2再与磺酰氯反应制得目标化合物.采用2倍稀释法对目标物进行体外抗菌活性筛选.结果 合成了16个结构新颖的蛇床子素磺酸酯衍生物,经核磁共振波谱法...

Synthesis and Antibacterial Activities of Novel Osthole Sulfonate Derivatives

OBJECTIVE To carry out stucture modification and bioactivity evaluation of natural product osthole in order to search for candidate antibacterial compounds. METHODS Using osthole as raw material, the intermediates 1 were synthesized by selenium dioxide oxidation, and the intermediates 2 were synthesized by reduction with sodium borohydride. A series of osthol sulfonic ester derivatives were synthesized by reaction of intermediate 2 with sulfonyl chloride. And the antibacterial activities of the products were evaluated by agar dilution method. RESULTS Sixteen title compounds were synthesized, and their structures were clearly elucidated by NMR and MS. The results showed that osthole derivatives had potential activities against the tested bacteria. The MIC of compound 3 p against S.aureu and MRSA were 32, 32 μg·mL^-1, respectively. The anti-S.aureu activity was significantly better than osthole, close to that of oxacillin, while the activity of anti-MRSA was much higher than those of osthole and oxacillin. CONCLUSION The sulfonate derivatives of osthole are significantly active against MRSA, which are worthy of further structural optimization and study.