ArticleDaru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences2020
Design, synthesis, molecular docking study, and antibacterial evaluation of some new fluoroquinolone analogues bearing a quinazolinone moiety.
Article in Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers, 1 of them a synthesis that pooled it.
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Who cites it
5 citing papers in PubMed, 1 synthesis or guideline pooled it, 22 citations in OpenAlex.
- A Systematic Review of Synthetic and Anticancer and Antimicrobial Activity of Quinazoline/Quinazolin-4-one Analogues.ChemistryOpen · 2025Pooled it
- The Difluoroboranyl-Fluoroquinolone Derivative "7a" Inhibits Bacterial DNA Gyrase and Exhibits Potent Activity Against Ciprofloxacin-ResistantMolecules (Basel, Switzerland) · 2026Article
- The Derivative Difluoroboranyl-Fluoroquinolone "7a" Generates Effective Inhibition Against theCurrent issues in molecular biology · 2025Article
- Novel Fluoroquinolones with Possible Antibacterial Activity in Gram-Negative Resistant Pathogens: In Silico Drug Discovery.Molecules (Basel, Switzerland) · 2023Article
- Photothermal card reader assay using the commercial colloidal gold test strip for the rapid quantitative detection of food hazards.Mikrochimica acta · 2022Article
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Authors and funding
8 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundIncreasing bacterial resistance to quinolones is concerning. Hence, the development of novel quinolones by chemical modifications to overcome quinolone resistance is an attractive perspective in this context.
objectiveIn this study, it is aimed to design and synthesize a novel series of functionalized fluoroquinolones using ciprofloxacin and sarafloxacin cores by hybridization of quinazolinone derivatives. This objective was tested by a comprehensive set of in vitro antibacterial assays in addition to SAR (structure-activity relationship) characterisation studies.
methodsA nucleophilic reaction of ciprofloxacin and sarafloxacin with 2-(chloromethyl)quinazolin-4(3H)-one in the presence of NaHCO
resultsThe compounds exhibited moderate to good activities against gram-positive bacteria and weak to moderate activities against gram-negative bacteria. Amongst all ciprofloxacin-derivatives, compound 5d was the most potent agent with high antibacterial activity against gram-positive bacteria, including MRSA and S. aureus ((minimum inhibitory concentration (MIC) = 16 nM for both), that is 60 times more potent than ciprofloxacin as parent drug. Compound 5i from sarafloxacin-derivatives was the most potent compound against MRSA and S. aureus (MIC = 0.125 μM). Well diffusion and disk diffusion assay results demonstrated confirmatory outcomes for the quantitative broth microdilution assay. Molecular docking study results were in accordance with the results of antibacterial activity assays.
conclusionThe results of the current study demonstrated that the novel ciprofloxacin and sarafloxacin derivatives synthesized here have promising antibacterial activities. Particularly, compounds 5d and 5i have potential for wider antibacterial applications following further analysis.
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