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Peer-reviewedCC BY 4.0Molecules

Quinolone Antimicrobials: A Medicinal Chemistry Perspective on Structural Evolution, Pharmacology, and Computational Profiling

  • Gustavo Machado das Neves1,2
  • Graziela de Araújo Lock3
  • Itamar Luís Gonçalves4
  • Teresa Cristina Tavares Dalla Costa5
  • Vera Lucia Eifler-Lima1
5 affiliations
  1. 1Medicinal Organic Synthesis Laboratory (LaSOM®), Pharmaceutical Sciences Graduate Program, Faculty of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre 90610-000, Brazil
  2. 2Faculty of Medicine, Federal University of Rio Grande, Rio Grande 96200-200, Brazil
  3. 3Department of Pharmacy, Health Sciences Centre, Federal University of Santa Maria, Santa Maria 97105-900, Brazil
  4. 4Graduate Program in Integral Health Care (UNICRUZ/URI-Erechim/UNIJUÍ), Integrated Regional University of Alto Uruguai e das Missões, Erechim 99709-910, Brazil
  5. 5Pharmacokinetics and PK/PD Modeling Laboratory, Faculty of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre 90610-000, Brazil
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Abstract

Quinolones are among the most successful antibacterial drugs developed in the last century. These drugs act selectively by inhibiting bacterial type II topoisomerases (DNA gyrase and topoisomerase IV), thereby impairing DNA replication and transcription. In the more than sixty years since the first quinolone entered the market, several others have been developed and classified into four generations according to their chemical modifications and effects on the spectrum of antibacterial activity. This review aims to provide an updated overview on this class of antimicrobials for scientists and clinicians doing research in the field of quinolones. We considered perspectives from several areas of medicinal chemistry, including the historical development and chemical evolution of quinolones, as well as their pharmacodynamics and mechanism of action, pharmacokinetics, and toxicity. Additionally, we integrated modern computational and analytical approaches, including bibliometric analysis, molecular docking, and drug-likeness profiling of quinolones to further understand their evolution and development.

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Cite

BibTeXRIS
BibTeX
@article{neves2026quinolone,
  title = {{Quinolone Antimicrobials: A Medicinal Chemistry Perspective on Structural Evolution, Pharmacology, and Computational Profiling}},
  author = {Gustavo Machado das Neves and Graziela de Araújo Lock and Itamar Luís Gonçalves and Teresa Cristina Tavares Dalla Costa and Vera Lucia Eifler-Lima},
  journal = {Molecules},
  year = {2026},
  month = nov,
  doi = {10.3390/molecules31213949},
  url = {https://www.mdpi.com/1420-3049/31/21/3949},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - Quinolone Antimicrobials: A Medicinal Chemistry Perspective on Structural Evolution, Pharmacology, and Computational Profiling
AU  - Gustavo Machado das Neves
AU  - Graziela de Araújo Lock
AU  - Itamar Luís Gonçalves
AU  - Teresa Cristina Tavares Dalla Costa
AU  - Vera Lucia Eifler-Lima
PY  - 2026
DA  - 2026/11/02
JO  - Molecules
DO  - 10.3390/molecules31213949
UR  - https://www.mdpi.com/1420-3049/31/21/3949
AB  - Quinolones are among the most successful antibacterial drugs developed in the last century. These drugs act selectively by inhibiting bacterial type II topoisomerases (DNA gyrase and topoisomerase IV), thereby impairing DNA replication and transcription. In the more than sixty years since the first quinolone entered the market, several others have been developed and classified into four generations according to their chemical modifications and effects on the spectrum of antibacterial activity. This review aims to provide an updated overview on this class of antimicrobials for scientists and clinicians doing research in the field of quinolones. We considered perspectives from several areas of medicinal chemistry, including the historical development and chemical evolution of quinolones, as well as their pharmacodynamics and mechanism of action, pharmacokinetics, and toxicity. Additionally, we integrated modern computational and analytical approaches, including bibliometric analysis, molecular docking, and drug-likeness profiling of quinolones to further understand their evolution and development.
SN  - 1420-3049
ER  -