Design, Synthesis, Antibacterial Evaluation and Docking Study of Novel 2-Hydroxy-3-(nitroimidazolyl)-propyl-derived Quinolone

作者：Li, Qing; Xing, Junhao; Cheng, Haibo; Wang, Hui; Wang, Jing; Wang, Shuai; Zhou, Jinpei; Zhang, Huibin^*

来源：Chemical Biology & Drug Design, 2015, 85(1): 79-90.

DOI：10.1111/cbdd.12395

• antibacterial activity
• docking study
• nitroimidazole
• quinolone

A novel series of 2-hydroxy-3-(nitroimidazolyl)-propyl-derived quinolones 6a-o were synthesized and evaluated for their in vitro antibacterial activity. Most of the target compounds exhibited potent activity against Gram-positive strains. Among them, moxifloxacin analog 6n displayed the most potent activity against Gram-positive strains including S.epidermidis (MIC=0.06g/mL), MSSE (MIC=0.125g/mL), MRSE (MIC=0.03g/mL), S.aureus (MIC=0.125g/mL), MSSA (MIC=0.125g/mL), (MIC=2g/mL). Its activity against MRSA was eightfold more potent than reference drug gatifloxacin. Finally, docking study of the target compound 6n revealed that the binding model of quinolone nucleus was similar to that of gatifloxacin and the 2-hydroxy-3-(nitroimidazolyl)-propyl group formed two additional hydrogen bonds.

• 出版日期2015-1
• 单位中国药科大学