1. Novel fluoroquinolones analogues bearing 4-(arylcarbamoyl)benzyl: design, synthesis, and antibacterial evaluation.
- Author
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Peytam F, Norouzbahari M, Saadattalab T, Şanlıtürk G, Firoozpour L, Emamgholipour Z, Dogaheh MG, Nikou M, Tehrani MB, Bijanzadeh HR, Güran M, and Foroumadi A
- Subjects
- Structure-Activity Relationship, Gram-Negative Bacteria drug effects, DNA Gyrase metabolism, Gram-Positive Bacteria drug effects, Chemistry Techniques, Synthetic, Anti-Bacterial Agents pharmacology, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry, Fluoroquinolones pharmacology, Fluoroquinolones chemistry, Fluoroquinolones chemical synthesis, Microbial Sensitivity Tests, Drug Design, Molecular Docking Simulation
- Abstract
Bacterial resistance to fluoroquinolone has been increasing at an alarming rate worldwide. In an attempt to find more potent anti-bacterial agents, an efficient, straightforward protocol was performed to obtain a large substrate scope of novel ciprofloxacin and sarafloxacin analogues conjugated with 4-(arylcarbamoyl)benzyl 7a-ab. All prepared compounds were evaluated for their anti-bacterial activities against three gram-positive strains (Methicillin resistant staphylococcus aureus (MRSA), Staphylococcus aureus, and Enterococcus faecalis) as well as three gram-negative strains (Pseudomonas aeruginosa, Klebsiella pneumonia, and Escherichia coli) through three standard methods including broth microdilution, agar-disc diffusion, and agar-well diffusion assays. Most of the compounds exhibited great to excellent anti-bacterial potencies against MRSA and S. aureus. Among the targeted compounds, derivative 7n exhibited great antibacterial potency, which was noticeably more potent than parent ciprofloxacin. Subsequently, a molecular docking study was performed for this compound to find out its probable binding mode with the active site of S. aureus DNA gyrase (PDB ID: 2XCT)., (© 2023. The Author(s), under exclusive licence to Springer Nature Switzerland AG.)
- Published
- 2024
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