高等学校化学学报2024，Vol.45Issue(7)：68-77,10.DOI:10.7503/cjcu20240124
含(杂)芳磺酰基哌嗪的蛇床子素衍生物的合成及抗菌活性
Synthesis and Antibacterial Activities of Osthole Derivatives Containing(Hetero)arylsulfonylpiperazine
摘要
Abstract
In order to obtain antibacterial candidate compounds,the strategy of pharmacophore hybridisation was adopted to optimize the structure of the previously obtained active compound.Twenty-five osthole derivatives were designed and synthesized,and confirmed by means of nuclear magnetic resonance hydrogen spectroscopy(1H NMR),nuclear magnetic resonance carbon spectroscopy(13C NMR)and elemental analysis.The antibacterial activities against S.aureus,E.coli,methicillin-resistant S.aureus(MRSA)and fluoroquinolone-resistant E.coli(FREC)were evaluated,the results showed that the minimum inhibitory concentration(MIC)of compound 4q was 0.5,1,2,2 µg/mL respectively,the MIC of compound 4s was 0.25,0.5,1,2 µg/mL respectively,and the MIC of compound 4u was 0.5,2,1,4 µg/mL respectively.The inhibitory activities of these compounds against S.aureus were comparable to the control drug oxacillin,and superior to norfloxacin,and against E.coli,MRSA,and FREC were superior to the control drugs oxacillin and norfloxacin.The combination of(hetero)arylsulfonylpiperazine and osthole can effectively enhance antibacterial activities and expand the antibacterial spectrums.关键词
蛇床子素衍生物/哌嗪/磺酰胺/抗菌活性Key words
Osthole derivative/Piperazine/Sulfonamide/Antibacterial activity分类
化学化工引用本文复制引用
杨家强,吴学姣,卢子聪,陈阳密,佘慧娴,刘讴灵..含(杂)芳磺酰基哌嗪的蛇床子素衍生物的合成及抗菌活性[J].高等学校化学学报,2024,45(7):68-77,10.基金项目
贵州省科技计划项目(批准号:黔科合基础-ZK[2024]一般265)和国家级大学生创新创业训练计划项目(批准号:202310661006)资助.Supported by the Science and Technology Plan Project of Guizhou Province,China(No.Qiankehe Foundation ZK[2024]265)and the National College Students'Innovation and Entrepreneurship Training Program of China(No.202310661006). （批准号:黔科合基础-ZK[2024]一般265）
