Gutiérrez-Mauricio Alicia M, Trujillo-Paez Juan Valentín, Trejo-Martinez Luis Alberto, Rivas-Santiago Bruno, Pérez-García Paola, Noriega Saúl, López-Ramos Juan Ernesto, Cardoso-Ortiz Jaime, Rodríguez-Carlos Adrián
Unidad Académica de Ciencias Químicas, Universidad Autónoma de Zacatecas, Zacatecas, Mexico.
Biomedical Research Unit-Zacatecas, Mexican Institute for Social Security-IMSS, Zacatecas, Mexico.
J Antibiot (Tokyo). 2025 Jul 1. doi: 10.1038/s41429-025-00839-2.
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.
结核病（TB）是由结核分枝杆菌（Mtb）引起的一种传染性疾病。它通过活动性肺结核患者呼出的空气中的小颗粒（<5 µm）传播；当被新宿主吸入时，这些颗粒可能会导致感染。如今，结核病仍然是单一传染源导致发病和死亡的主要原因，全球范围内出现的耐多药结核分枝杆菌菌株进一步加剧了这一情况。因此，必须采取有效的诊断、预防方法以及新的药物治疗手段来控制这种疾病。氟喹诺酮类（FQ）是一类合成抗生素，对革兰氏阴性菌和革兰氏阳性菌具有广谱抗菌活性，包括结核分枝杆菌。FQ治疗在耐药结核病的管理中发挥着重要作用。人们对FQ结构的修饰进行了广泛研究，由此出现了四代具有广谱抗菌特性的FQ。这些修饰通过增加组织穿透力、减少副作用以及应对新出现的细菌耐药性来提高FQ的整体疗效。在这种情况下，当前FQ研究趋势集中在新的合成方法上，以使氟喹诺酮类能够应对全球耐多药结核病问题。本综述的目的是突出具有抗结核活性的新合成FQ分子的总体效果。
