Abstract��OBJECTIVE To search more effective antibacterial candidate agents by designing a series of 7-phosphoryl quinolone derivatives,exploring the synthetic methods, and evaluating their antibacterial activities. METHODS The quinolone derivatives were synthesized using phosphate and quinolone intermediates as raw materials and alkaline ionic liquid [Bmim] OH as catalyst with microwave assistance. The antibacterial activities of the products were evaluated by agar dilution method. RESULTS Eight title compounds were prepared, and their structures were clearly established by IR, NMR and MS. The in vitro experiment showed that the derivatives had potential antibacterial activity. Especially, compound ��c showed more potent activities against S. aureus, E. coli, MREC-1# and MREC-2# with minimum inhibitory concentrations (MICs) of 1.6, 6.4, 12.8,6.4 mg��mL-1, respectively, and the MICs of compound �� gagainst S. aureus, E. coli, MREC-1# and MREC-2# were 1.6, 3.2, 6.4, 6.4 mg��mL-1, respectively. Its activity on drug-resistant bacteria was better than that of the control drug norfloxacin. CONCLUSION The quinolone derivatives are highly active on drug-resistant bacteria.It is worth of further study.
���ǿ, ������, ��ά, ��ٻ. 7-�������ŵͪ������ĺϳ��뿹�������о�[J]. �й�ҩѧ��־, 2019, 54(2): 86-90.
YANG Jia-qiang, CHE Wan-li, WANG Wei, LI Qian. Synthesis and Antibacterial Activity of Novel 7-Phosphoryl Quinolone Derivatives. Chinese Pharmaceutical Journal, 2019, 54(2): 86-90.
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2019, Vol. 54 
