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Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors.
- Source :
- Pharmaceuticals (14248247); May2021, Vol. 14 Issue 5, p399, 1p
- Publication Year :
- 2021
-
Abstract
- A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been synthesized and structurally elucidated using <superscript>1</superscript>H NMR, <superscript>13</superscript>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<subscript>50</subscript> of 86, 42, 92, and 180 nM against E. coli DNA gyrase, respectively (novobiocin, IC<subscript>50</subscript> = 170 nM). Compounds 4, 5, and 6 showed IC<subscript>50</subscript> values (1.47, 6.80, and 8.92 µM, respectively) against E. coli topo IV in comparison to novobiocin (IC<subscript>50</subscript> = 11 µM). [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14248247
- Volume :
- 14
- Issue :
- 5
- Database :
- Complementary Index
- Journal :
- Pharmaceuticals (14248247)
- Publication Type :
- Academic Journal
- Accession number :
- 150502158
- Full Text :
- https://doi.org/10.3390/ph14050399