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A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been synthesized and structurally elucidated using  1 H NMR,  13 C NMR, and elementary analyses. Using ciprofloxacin as a reference, compounds  1–21  were screened in vitro against Gram-positive bacterial strains such as  Staphylococcus aureus  and  Bacillus subtilis  and Gram-negative strains such as  Escherichia coli  and  Pseudomonas aeruginosa . As a result, many of the compounds examined had antibacterial activity equivalent to ciprofloxacin against test bacteria. Compounds  2–6 , oxadiazole derivatives, were found to have antibacterial activity that was 88 to 120% that of ciprofloxacin against Gram-positive and Gram-negative bacteria. The findings showed that none of the compounds tested had antifungal activity against  Aspergillus flavus , but did have poor activity against  Candida albicans , ranging from 23% to 33% of fluconazole, with compound  3  being the most active (33% of fluconazole). The most potent compounds,  3 ,  4 ,  5 , and  6 , displayed an IC 50  of 86, 42, 92, and 180 nM against  E. coli  DNA gyrase, respectively (novobiocin, IC 50  = 170 nM). Compounds  4 ,  5 , and  6  showed IC 50  values (1.47, 6.80, and 8.92 µM, respectively) against  E. coli  topo IV in comparison to novobiocin (IC 50  = 11 µM).

Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors