In vitro activities of a new fluoroquinolone derivative highly active against Chlamydia trachomatis

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TitreIn vitro activities of a new fluoroquinolone derivative highly active against Chlamydia trachomatis
Type de publicationJournal Article
Year of Publication2019
AuteursVu THuyen, Ha-Duong N-T, Aubry A, Capton E, Fechter P, Plesiat P, Verbeke P, Serradji N
JournalBIOORGANIC CHEMISTRY
Volume83
Pagination180-185
Date PublishedMAR
Type of ArticleArticle
ISSN0045-2068
Mots-clés8-Hydroxyquinoline, Ciprofloxacin, Gram-negative, Gram-positive, inhibitors
Résumé

Chlamydia trachomatis is a bacterial human pathogen responsible for the development of trachoma, an infection leading to blindness, and is also the cause of the main bacterial sexually transmitted infection worldwide. We designed a new inhibitor of this bacterium with, however, some prerequisites using (i) the iron dependency of the bacterium, (ii) a commercially available broad-spectrum antibiotic and (iii) a short synthetic pathway. The corresponding 8-hydroxyquinoline-ciprofloxacin conjugate was evaluated against a panel of pathogenic bacteria, including C. trachomatis but also the ESKAPE group (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and Enterobacter species). Its anti-Chlamydia activity is higher than that of ciprofloxacin and seems to be related to the fluoroquinolone moiety of the molecule, which is also responsible for the complexation of iron(III), as demonstrated by spectrophotometric titration.

DOI10.1016/j.bioorg.2018.10.033