AIM: To study the synthesis and antibacterial activity of ciprofloxacin derivatives. METHODS: Ciprofloxacin derivatives were synthesized primarily from 2-methyl-5-nitroimidazol and ciprofloxacin through nucleophilic substitution. The antibacterial activity of the synthesized compounds were tested. RESULTS: Nine new compounds were synthesized. The structure of the title compounds were confirmed by 1H NMR, MS and element analysis. CONCLUSION: Compounds II, IVC and IVD showed appreciable antibacterial activity, and were worth further studying.