Synthesis and Antibacterial Activity of Novel 7-Phosphoryl Quinolone Derivatives / 中国药学杂志

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 Ⅱc 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 Ⅱ 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.