Fluoroquinolone Derivatives in the Treatment of Mycobacterium tuberculosis Infection.

Détails

Ressource 1Télécharger: 36297325_BIB_9968C11BE9CE.pdf (1901.21 [Ko])
Etat: Public
Version: Final published version
Licence: CC BY 4.0
ID Serval
serval:BIB_9968C11BE9CE
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
Fluoroquinolone Derivatives in the Treatment of Mycobacterium tuberculosis Infection.
Périodique
Pharmaceuticals
Auteur⸱e⸱s
Pais J.P., Policarpo M., Pires D., Francisco A.P., Madureira A.M., Testa B., Anes E., Constantino L.
ISSN
1424-8247 (Print)
ISSN-L
1424-8247
Statut éditorial
Publié
Date de publication
30/09/2022
Peer-reviewed
Oui
Volume
15
Numéro
10
Pages
1213
Langue
anglais
Notes
Publication types: Journal Article
Publication Status: epublish
Résumé
Tuberculosis (TB) is currently one of the leading causes of death due to infective agents, and the growing rate of multidrug-resistant tuberculosis (MDR TB) cases poses an emergent public health threat. Fluoroquinolones are commonly used in the treatment of both MDR TB and drug-sensitive tuberculosis patients who are intolerant to first-line antitubercular agents. Unfortunately, these drugs have mild side effects, relevant to the prolonged treatment regimens and diminished bioavailability due to binding of metal ions. Moreover, the resistance to fluoroquinolones is also on the rise, a characteristic of extensively drug-resistant TB (XDR TB). Here, we developed esters as prodrugs of the fluoroquinolones levofloxacin and ciprofloxacin, with long-chain fatty alcohols. Both the alcohols and the quinolone have previously shown antimycobacterial activity and the aim was to develop esters with improved lipophilicity and capable of delivering the free acid inside mycobacterial cells. The carboxylic acid group of fluoroquinolones is essential to the mode of action but is also responsible for many of its side effects and metal-chelating properties. The synthesis, stability in biological media, and antibacterial activity were evaluated, the latter not only against Mycobacterium tuberculosis but also against other clinically relevant bacterial species, since the parent compounds display a broad spectrum of activity. The biological results show a reduction in the antitubercular activity of the synthesized derivatives, probably due to deficient activation of the ester prodrug. Despite this, it was found that the derivatives exhibit bioactivity against other fluoroquinolone-resistant bacteria, indicating a different mode of action and suggesting that it may be worthwhile to research further modifications to the carboxylic acid group. This might lead to new compounds that are efficient against resistant strains. This idea that the compounds may act by a different mechanism of action was further supported by a brief computer investigation that demonstrated the potential lack of selectivity of the esters to the fluoroquinolone target.
Mots-clé
esters, fluoroquinolones, mycobacteria, prodrugs, tuberculosis
Pubmed
Web of science
Open Access
Oui
Création de la notice
08/11/2022 12:09
Dernière modification de la notice
23/01/2024 7:30
Données d'usage