Novel Fluoroquinolones Analogues Bearing 4-(Arylcarbamoyl)Benzyl: Design, Synthesis, and Antibacterial Evaluation Publisher



Peytam F¹ ; Norouzbahari M^{2, 3} ; Saadattalab T⁴ ; Sanliturk G⁵ ; Firoozpour L⁶ ; Emamgholipour Z⁶ ; Dogaheh MG⁶ ; Nikou M⁶ ; Tehrani MB⁶ ; Bijanzadeh HR⁷ ; Guran M² ; Foroumadi A^{1, 6}
Source: Molecular Diversity Published:2023

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.