In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives
Antibacterial activity; Fluoroquinolones; Minimal inhibitory concentration; Norfloxacin 7 hydrazinoquinolone; 7 substituted 6 fluoroquinolone; 7 substituted 6,8 difluoroquinolone; balofloxacin; ciprofloxacin; garenoxacin; moxifloxacin; norfloxacin; quinoline derived antiinfective agent; rosoxacin; unclassified drug; antiinfective agent; quinolone derivative; antibacterial activity; antibiotic sensitivity; Article; Bacillus subtilis; bacterial growth; disk diffusion; Enterococcus faecalis; Escherichia coli; in vitro study; incubation time; minimum inhibitory concentration; nonhuman; priority journal; Pseudomonas aeruginosa; Staphylococcus aureus; structure activity relation; chemistry; drug effects; Gram negative bacterium; Gram positive bacterium; microbial sensitivity test; Anti-Bacterial Agents; Fluoroquinolones; Gram-Negative Bacteria; Gram-Positive Bacteria; Microbial Sensitivity Tests; Quinolones; Structure-Activity Relationship
Background: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. Methods: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method. Minimal inhibitory concentration (MIC) was determined by measuring the diameter of the inhibition zone using concentrations between 250 and 0.004 μg/mL. Results: MIC of derivatives 2, 3, and 4 showed potent antimicrobial activity against gram-positive and gram-negative bacteria. The effective concentrations were 0.860 μg/mL or lower. MIC for compounds 5-11 were between 120 and 515 μg/mL against Escherichia coli and Staphylococcus aureus, and substituted hydrazinoquinolones 7-10 showed poor antibacterial activity against gram-positive and gram-negative bacteria compared with other quinolones. Conclusion: Compounds obtained by modifications on C-7 of norfloxacin with the acetylated piperazinyl, halogen atoms, and substituted hydrazinyl showed good in vitro activity-some even better than the original compound. © 2017 S. Karger AG, Basel.
balofloxacin, 127294-70-6; ciprofloxacin, 85721-33-1; garenoxacin, 194804-75-6, 223652-82-2, 223652-90-2; moxifloxacin, 151096-09-2; norfloxacin, 70458-96-7; rosoxacin, 40034-42-2; Anti-Bacterial Agents; Fluoroquinolones; Quinolones
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