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

被引：14

作者：

Thi Huyen Vu ^{[1
,2
]}

Nguyet-Thanh Ha-Duong ^{[1
]}

Aubry, Alexandra ^{[3
,4
]}

Capton, Estelle ^{[4
]}

Fechter, Pierre ^{[5
,6
]}

Plesiat, Patrick ^{[7
]}

Verbeke, Philippe ^{[8
]}

Serradji, Nawal ^{[1
]}

机构：

[1] Univ Paris Diderot, CNRS, ITODYS, Sorbonne Paris Cite,UMR 7086, 15 Rue Jean Antoine de Baif, F-75205 Paris, France

[2] USTH, Vietnam Acad Sci & Technol, 18 Hoang Quoc Viet, Hanoi, Vietnam

[3] Hop La Pitie Salpetriere, AP HP, Ctr Natl Reference Mycobacteries & Resistance Myc, F-75013 Paris, France

[4] Sorbonne Uni, INSERM, Ctr Immunol & Malad Infect, Cimi Paris,Equipe 13,U1135, F-13 Paris, France

[5] CNRS, UMR 7242, Biotechnol & Signalisat Cellulaire, F-67400 Illkirch Graffenstaden, France

[6] Univ Strasbourg, Inst Rech, Ecole Biotechnol Strasbourg, F-67400 Illkirch Graffenstaden, France

[7] Hop Jean Minjos, Ctr Natl Reference Resistance Antibiot, Blvd Fleming, F-25030 Besancon, France

[8] Univ Paris Diderot, Fac Med Xavier Bichat, INSERM U1149, Sorbonne Paris Cite, 16 Rue Henri Huchard, F-75018 Paris, France

来源：

BIOORGANIC CHEMISTRY | 2019年 / 83卷

关键词：

Inhibitors; 8-Hydroxyquinoline; Ciprofloxacin; Gram-negative; Gram-positive; DNA GYRASE; WOMEN; CIPROFLOXACIN; PERSISTENCE; INFECTIONS; PNEUMONIAE; RESISTANCE; INHIBITORS; DESIGN; AGENTS;

D O I：

10.1016/j.bioorg.2018.10.033

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：180 / 185

页数：6

共 33 条

[1] Design and synthesis of 3-isoxazolidone derivatives as new Chlamydia trachomatis inhibitors [J].