Antibacterial Activity of Quinolone Derivatives
Summary
Quinolone derivatives represent a cornerstone of modern antibacterial chemotherapy, characterised by a bicyclic core that can be variably substituted to modulate spectrum, potency and pharmacokinetic properties. Fluoroquinolones, distinguished by a fluorine atom at the C-6 position, inhibit bacterial type II topoisomerases—primarily DNA gyrase and topoisomerase IV—thereby blocking DNA replication and transcription. Over successive generations, modifications at key positions (notably C-3, C-7 and N-1) have yielded agents with improved activity against Gram-negative and Gram-positive pathogens, enhanced tissue penetration and favourable oral bioavailability. However, the rise of resistant strains and the persistence of biofilms on medical devices remain pressing challenges. Contemporary efforts focus on novel derivatives that combine potent enzyme inhibition with additional mechanisms—such as membrane disruption or antibiofilm activity—and on hybrid molecules that may delay resistance emergence. These advances hold promise for global health by addressing complicated infections, reducing treatment failures and informing the next generation of antibacterial agents.
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Antibacterial Activity of Quinolone Derivatives publication trend
The graph below shows the total number of articles in antibacterial activity of quinolone derivatives across all publications each year (not limited to Nature Index journals).
Technical terms
Quinolone: Core bicyclic scaffolds that serve as the basis for a class of synthetic antibacterials.
Fluoroquinolone: Quinolone derivatives bearing a fluorine atom, which enhance potency and spectrum of activity.
Minimum inhibitory concentration (MIC): Lowest concentration of an antibacterial agent that prevents visible growth of a microorganism under standardized conditions.
Biofilm: Structured communities of bacteria adhered to surfaces and embedded in an extracellular polymeric matrix, often refractory to treatment.
DNA gyrase: Bacterial topoisomerase that introduces negative supercoils into DNA, crucial for replication and a primary target of quinolone derivatives.
Structure–activity relationship (SAR): Analysis linking chemical structure modifications to changes in biological activity, guiding rational drug design.
References
- Antibacterial and antibiofilm activity of permanently ionized quaternary ammonium fluoroquinolones. European Journal of Medicinal Chemistry (2023).
- A Comprehensive Review on Chemical Synthesis and Chemotherapeutic Potential of 3-Heteroaryl Fluoroquinolone Hybrids. Antibiotics (2023).
- Advances in the Synthesis and Biological Applications of Enoxacin-Based Compounds. Biomolecules (2024).
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