Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 85, Issue 1, Pages 79-90Publisher
WILEY
DOI: 10.1111/cbdd.12395
Keywords
antibacterial activity; docking study; nitroimidazole; quinolone
Funding
- China National Key Hi-Tech Innovation Project for the R&D of Novel Drugs [2013ZX09301303-002]
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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.
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