New ciprofloxacin–dithiocarbamate–benzyl hybrids: design, synthesis, antibacterial evaluation, and molecular modeling studies
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We designed and synthesized a series of new ciprofloxacin–dithiocarbamate–benzyl hybrids 5a–n as potential antibacterial agents. All of the synthesized compounds were screened for in vitro antibacterial activity against four bacterial strains (Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, and Pseudomonas aeruginosa). The antibacterial results indicated that some of the synthesized compounds showed remarkable activity, comparable to their parent drug ciprofloxacin. Among the synthesized compounds, the 4-nitro derivative 5n, exhibited the most antibacterial activity against S. aureus, S. epidermidis, and E. coli. The antibacterial activity of this compound against S. aureus and E. coli was twofold higher than that of its parent ciprofloxacin. Molecular modeling of compound 5n was also investigated in the active site of E. coli DNA gyrase.
KeywordsCiprofloxacin Dithiocarbamate Docking study Antibacterial activity
This research was supported by grants from the research council of Tehran University of Medical Sciences and INSF (Iran National Science Foundation).
Compliance with ethical standards
Conflict of interest
The authors have declared no conflict of interest.
- 10.M.L. Liu, H.Y. Guo, World Notes Antibiot. 27, 69 (2006)Google Scholar
- 23.G. Cascio, L. Lorenzi, D. Caglio, E. Manghisi, F. Arcamone, G. Guanti, G. Satta, G. Morandotti, R. Sperning, Farmaco 51, 189 (1996)Google Scholar
- 24.E.J. Baron, S.M. Finegold, Diagn. Microbiol. 171 (1990)Google Scholar