含(杂)芳磺酰基哌嗪的蛇床子素衍生物的合成及抗菌活性OA北大核心CSTPCD

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.