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Tuberculosis drug development; fluoroquinolone structural tailoring

The Journal of Antibiotics volume 78, pages 517–534 (2025)Cite this article

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Abstract

Tuberculosis (TB) is a contagious infectious disease caused by the bacillus Mycobacterium tuberculosis (Mtb). It is transmitted through small particles in the air (<5 µm) expelled by active tuberculosis patients; when inhaled by a new host, they can potentially cause infection. Nowadays, TB is still the major cause of morbidity and mortality by a single infectious agent, this is further exacerbated by the worldwide emergence of multidrug-resistant strains of Mtb. Thus, effective methods of diagnosis, prophylaxis, and new pharmacological therapies must be carried out in order to control this disease. Fluoroquinolones (FQ) are synthetic antibiotics with a broad spectrum against Gram-negative and Gram-positive bacteria, including M. tuberculosis. The treatment with FQ plays an important role in managing drug-resistant tuberculosis. Modifications on FQ structure have been extensively studied, thereby, four generations of FQ have emerged having a broad spectrum of antibacterial properties. These modifications improve the overall efficiency of FQ by increasing tissue penetration, reducing side effects, and addressing emerging bacterial resistance. In this scenario, current trends on FQ research have focused on new synthetic approaches that allow fluoroquinolones to address the worldwide issue of multidrug-resistant tuberculosis. The aim of this review is to highlight the overall effects of newly synthesized FQ molecules having antitubercular activity.

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Acknowledgements

AMGM had a scholarship by SECIHTI (CVU:1325935).

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  1. These authors contributed equally: Alicia M. Gutiérrez-Mauricio, Juan Valentín Trujillo-Paez.

Authors and Affiliations

  1. Unidad Académica de Ciencias Químicas, Universidad Autónoma de Zacatecas, Zacatecas, Mexico

    Alicia M. Gutiérrez-Mauricio, Saúl Noriega & Jaime Cardoso-Ortiz

  2. Biomedical Research Unit-Zacatecas, Mexican Institute for Social Security-IMSS, Zacatecas, Mexico

    Alicia M. Gutiérrez-Mauricio, Bruno Rivas-Santiago, Paola Pérez-García & Adrián Rodríguez-Carlos

  3. CONAHCYT- Biomedical Research Unit-Zacatecas, Mexican Institute for Social Security-IMSS, Zacatecas, Mexico

    Juan Valentín Trujillo-Paez

  4. Oncólogico Potosino, Clinical Reseach Site, San Luis Potosí, SLP, Mexico

    Luis Alberto Trejo-Martinez

  5. Centro de Estudios Científicos y Tecnológicos 18 Zacatecas, Instituto Politécnico Nacional, Zacatecas, Mexico

    Juan Ernesto López-Ramos

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Gutiérrez-Mauricio, A.M., Trujillo-Paez, J.V., Trejo-Martinez, L.A. et al. Tuberculosis drug development; fluoroquinolone structural tailoring. J Antibiot 78, 517–534 (2025). https://doi.org/10.1038/s41429-025-00839-2

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