蛇床子素醚类衍生物的合成及抗菌活性

Synthesis and antibacterial activities of osthole ether derivatives

为了寻找抗菌先导化合物,以蛇床子素为原料,对其7位进行结构改造,经脱甲基化、醚化,设计合成了15个目标化合物,经^(1)H NMR、^(13)C NMR和MS对化合物进行结构确证。抗菌活性测试结果表明:该类衍生物对革兰氏阴性菌大肠杆菌(E.coli)有较好的抑制活性,其中,尤以化合物Ⅱb〔8-异戊烯基-7-环丙甲氧基香豆素〕的活性最为显著,对E.coli的最小抑菌浓度(MIC)为32 mg·L^(-1),远优于蛇床子素的活性,接近对照药苯唑西林(MIC=16 mg·L^(-1))的活性。该类衍生物的潜在抗菌活性,值得进一步结构优化和深入研究。

In order to find antibacterial lead compounds,fifteen target compounds were designed and synthesized from osthole by demethylation and etherification.The structures of the compounds were confirmed by ^(1)H NMR,^(13)C NMR and MS.The results showed that these derivatives had good inhibitory activities against E.coli,especially compound IIb[8-isopentenyl-7-cyclopropylmethoxycoumarin]was the most significant,and the MIC(minimum inhibitory concentration)against E.coli was 32 mg·L^(-1),which was much better than osthole(MIC=1024 mg·L^(-1)),and was close to that of the control drug oxacillin(MIC=16 mg·L^(-1)).The potential antibacterial activities of the derivatives should be further studied.