Summary: A group of QUINOLONES with at least one fluorine atom and a piperazinyl group.

Top Publications

  1. Hu Y, Hoffner S, Wu L, Zhao Q, Jiang W, Xu B. Prevalence and genetic characterization of second-line drug-resistant and extensively drug-resistant Mycobacterium tuberculosis in Rural China. Antimicrob Agents Chemother. 2013;57:3857-63 pubmed publisher
    ..Of 43 multidrug-resistant M. tuberculosis isolates, 13 showed resistance to fluoroquinolones or injectable second-line drugs (preextensively drug-resistant TB [pre-XDR-TB]), and 4 were resistant to both ..
  2. Qin P, Liu R. Oxidative stress response of two fluoroquinolones with catalase and erythrocytes: a combined molecular and cellular study. J Hazard Mater. 2013;252-253:321-9 pubmed publisher
    Ciprofloxacin (CPFX) and enrofloxacin (ENFX), two representatives of fluoroquinolones (FQs), pose potential threats to health for their wide exposures in environment...
  3. Guerrini V, De Rosa M, Pasquini S, Mugnaini C, Brizzi A, Cuppone A, et al. New fluoroquinolones active against fluoroquinolones-resistant Mycobacterium tuberculosis strains. Tuberculosis (Edinb). 2013;93:405-11 pubmed publisher
    A set of 21 new fluoroquinolones bearing an aromatic or heteroaromatic moiety at C-7 and an alkyl group at N-1 were synthesized based on the lead structure of pirfloxacin and tested in vitro against Mycobacterium tuberculosis (M...
  4. Zhang F, Gu S, Ding Y, Zhang Z, Li L. A novel sensor based on electropolymerization of β-cyclodextrin and L-arginine on carbon paste electrode for determination of fluoroquinolones. Anal Chim Acta. 2013;770:53-61 pubmed publisher
    An electrochemical sensor for fluoroquinolones (FQs) based on polymerization of β-cyclodextrin (β-CD) and L-arginine (L-arg) modified carbon paste electrode (CPE) (P-β-CD-L-arg/CPE) was built for the first time...
  5. Wu X, Chen H, Jiang H, Xu Y, Liu T, Xu L. Prophylactic effect of topical fluoroquinolones in a rabbit model of Staphylococcus aureus endophthalmitis. J Ocul Pharmacol Ther. 2012;28:186-93 pubmed publisher
    ..There was no difference, however, among the 4 fluoroquinolone-treated groups. In contrast, none of the fluoroquinolones reduced the number of bacteria recovered (CFUs) from the vitreous humor...
  6. Shi Y, Gao L, Li W, Liu J, Cai Y. Investigation of fluoroquinolones, sulfonamides and macrolides in long-term wastewater irrigation soil in Tianjin, China. Bull Environ Contam Toxicol. 2012;89:857-61 pubmed publisher
    b>Fluoroquinolones, sulfonamides and macrolides were analyzed in soil samples collected from suburban areas in Tianjin, China. Fluoroquinolones were the predominant class of antibiotics. The mean total concentration of fluoroquinolones (33...
  7. Biedenbach D, Turner L, Jones R, Farrell D. Activity of JNJ-Q2, a novel fluoroquinolone, tested against Neisseria gonorrhoeae, including ciprofloxacin-resistant strains. Diagn Microbiol Infect Dis. 2012;74:204-6 pubmed publisher
    ..06 ?g/mL) followed by JNJ-Q2 (MIC(90), 0.25 ?g/mL). JNJ-Q2 appears to be a potent fluoroquinolone when tested against contemporary multidrug-resistant N. gonorrhoeae. ..
  8. Suzuki Y, Nakajima C, Tamaru A, Kim H, Matsuba T, Saito H. Sensitivities of ciprofloxacin-resistant Mycobacterium tuberculosis clinical isolates to fluoroquinolones: role of mutant DNA gyrase subunits in drug resistance. Int J Antimicrob Agents. 2012;39:435-9 pubmed publisher
    ..Double gyrA mutations as well as mutations in both gyrA and gyrB correlated with increased resistance to all fluoroquinolones.
  9. Koirala K, Thanh D, Thapa S, Arjyal A, Karkey A, Dongol S, et al. Highly resistant Salmonella enterica serovar Typhi with a novel gyrA mutation raises questions about the long-term efficacy of older fluoroquinolones for treating typhoid fever. Antimicrob Agents Chemother. 2012;56:2761-2 pubmed publisher
    As a consequence of multidrug resistance, clinicians are highly dependent on fluoroquinolones for treating the serious systemic infection typhoid fever...

More Information


  1. Maruri F, Sterling T, Kaiga A, Blackman A, van der Heijden Y, Mayer C, et al. A systematic review of gyrase mutations associated with fluoroquinolone-resistant Mycobacterium tuberculosis and a proposed gyrase numbering system. J Antimicrob Chemother. 2012;67:819-31 pubmed publisher
    ..tuberculosis isolates had mutations in DNA gyrase, but a substantial proportion did not. The proposed consensus numbering system can improve molecular detection of resistance and identification of novel mutations. ..
  2. O Brien D, McDonald A, Callan P, Robson M, Friedman N, Hughes A, et al. Successful outcomes with oral fluoroquinolones combined with rifampicin in the treatment of Mycobacterium ulcerans: an observational cohort study. PLoS Negl Trop Dis. 2012;6:e1473 pubmed publisher
  3. Miotto P, Cabibbe A, Mantegani P, Borroni E, Fattorini L, Tortoli E, et al. GenoType MTBDRsl performance on clinical samples with diverse genetic background. Eur Respir J. 2012;40:690-8 pubmed publisher
    ..The performances of the MTBDRsl in detecting resistance to fluoroquinolones (FQ), second-line injectable drugs (SLID), and ethambutol (EMB) on clinical isolates were similar (..
  4. Horvath A, Dobay O, Kardos S, Ghidán A, Toth A, Pászti J, et al. Varying fitness cost associated with resistance to fluoroquinolones governs clonal dynamic of methicillin-resistant Staphylococcus aureus. Eur J Clin Microbiol Infect Dis. 2012;31:2029-36 pubmed publisher
    ..The Ser80???Phe mutation in the grlA gene may have seriously compromised viability. Surprisingly silent nucleotide substitutions in the grlB gene seemed to impact fitness in derivatives of the ST30-MRSA-IV isolate. ..
  5. Sung L, Manji A, Beyene J, Dupuis L, Alexander S, Phillips R, et al. Fluoroquinolones in children with fever and neutropenia: a systematic review of prospective trials. Pediatr Infect Dis J. 2012;31:431-5 pubmed publisher
    There has been reluctance to use fluoroquinolones in children because of arthropathy in animal models; experience in pediatric fever and neutropenia (FN) has been limited...
  6. Wang L, Yuanshu Z, Yuhan Z, Yaojie -, Yingxia L. Mutant prevention concentrations of fluoroquinolones against Campylobacter jejuni isolated from chicken. Vet Microbiol. 2010;144:409-14 pubmed publisher
    ..These findings provide new insights into the development and mechanisms of FQ resistance in Campylobacter. ..
  7. Ferjani S, Saidani M, Ennigrou S, Hsairi M, Ben Redjeb S. Virulence determinants, phylogenetic groups and fluoroquinolone resistance in Escherichia coli isolated from cystitis and pyelonephritis. Pathol Biol (Paris). 2012;60:270-4 pubmed publisher
    The aim of this study is to assess the relation between virulence genotype, phylogenetic group and susceptibility to fluoroquinolones and the urinary tract infection type including pyelonephritis and cystitis due to Escherichia coli.
  8. Vallet C, Marquez B, Ngabirano E, Lemaire S, Mingeot Leclercq M, Tulkens P, et al. Cellular accumulation of fluoroquinolones is not predictive of their intracellular activity: studies with gemifloxacin, moxifloxacin and ciprofloxacin in a pharmacokinetic/pharmacodynamic model of uninfected and infected macrophages. Int J Antimicrob Agents. 2011;38:249-56 pubmed publisher
    b>Fluoroquinolones enter eukaryotic cells but the correlation between cellular accumulation and activity remains poorly established. Gemifloxacin is known to accumulate to a larger extent than most other fluoroquinolones in tissues...
  9. Kontsevaya I, Mironova S, Nikolayevskyy V, Balabanova Y, Mitchell S, Drobniewski F. Evaluation of two molecular assays for rapid detection of mycobacterium tuberculosis resistance to fluoroquinolones in high-tuberculosis and -multidrug-resistance Settings. J Clin Microbiol. 2011;49:2832-7 pubmed publisher
    ..Rapid diagnosis of resistance to fluoroquinolones (FQs) using molecular assays is essential for the implementation of appropriate drug regimens and prevention ..
  10. Costa S, Falcão C, Viveiros M, Machado D, Martins M, Melo Cristino J, et al. Exploring the contribution of efflux on the resistance to fluoroquinolones in clinical isolates of Staphylococcus aureus. BMC Microbiol. 2011;11:241 pubmed publisher
    ..a hospital in Lisbon, Portugal, in order to understand the role played by these systems in the resistance to fluoroquinolones. Augmented efflux activity was detected in 12 out of 52 isolates and correlated with increased resistance to ..
  11. Hu Y, Mathema B, Wang W, Kreiswirth B, Jiang W, Xu B. Population-based investigation of fluoroquinolones resistant tuberculosis in rural eastern China. Tuberculosis (Edinb). 2011;91:238-43 pubmed publisher
    Empirical use of fluoroquinolones (FQ) to treat a variety of bacterial infections may inadvertently select for FQ-resistant strains of Mycobacterium tuberculosis(MTB), especially in rural China where the use of FQ in treating infections ..
  12. Lemaire S, Tulkens P, Van Bambeke F. Contrasting effects of acidic pH on the extracellular and intracellular activities of the anti-gram-positive fluoroquinolones moxifloxacin and delafloxacin against Staphylococcus aureus. Antimicrob Agents Chemother. 2011;55:649-58 pubmed publisher
    In contrast to currently marketed fluoroquinolones, which are zwitterionic, delafloxacin is an investigational fluoroquinolone with an anionic character that is highly active against Gram-positive bacteria...
  13. Wispelwey B, Schafer K. Fluoroquinolones in the management of community-acquired pneumonia in primary care. Expert Rev Anti Infect Ther. 2010;8:1259-71 pubmed publisher
    ..search was conducted to evaluate the pharmacokinetic and pharmacodynamic profile of the respiratory fluoroquinolones (gemifloxacin, levofloxacin and moxifloxacin) and their efficacy and safety in the management of community-..
  14. El Garch F, Lismond A, Piddock L, Courvalin P, Tulkens P, Van Bambeke F. Fluoroquinolones induce the expression of patA and patB, which encode ABC efflux pumps in Streptococcus pneumoniae. J Antimicrob Chemother. 2010;65:2076-82 pubmed publisher
    Active efflux is a common mechanism of resistance to fluoroquinolones in Streptococcus pneumoniae...
  15. Yan H, Wang H, Qin X, Liu B, Du J. Ultrasound-assisted dispersive liquid-liquid microextraction for determination of fluoroquinolones in pharmaceutical wastewater. J Pharm Biomed Anal. 2011;54:53-7 pubmed publisher
    ..coupled with liquid chromatography-ultraviolet detection (LC-UV) was developed for the determination of four fluoroquinolones (ofloxacin, norfloxacin, enrofloxacin, and lomefloxacin) in pharmaceutical wastewater samples...
  16. Disratthakit A, Doi N. In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species. Antimicrob Agents Chemother. 2010;54:2684-6 pubmed publisher
    ..The anti-tubercle bacilli activity of DC-159a was 4- to 32-fold more potent than those of currently available quinolones. DC-159a also demonstrated the highest activities against clinically important nontuberculous mycobacteria. ..
  17. Caminero J, Sotgiu G, Zumla A, Migliori G. Best drug treatment for multidrug-resistant and extensively drug-resistant tuberculosis. Lancet Infect Dis. 2010;10:621-9 pubmed publisher
    ..The second group is the fluoroquinolones, of which the first choice is high-dose levofloxacin...
  18. Boulund F, Johnning A, Pereira M, Larsson D, Kristiansson E. A novel method to discover fluoroquinolone antibiotic resistance (qnr) genes in fragmented nucleotide sequences. BMC Genomics. 2012;13:695 pubmed publisher
    ..An implementation of the method is freely available at http://bioinformatics.math.chalmers.se/qnr/. ..
  19. Lau R, Ho P, Kao R, Yew W, Lau T, Cheng V, et al. Molecular characterization of fluoroquinolone resistance in Mycobacterium tuberculosis: functional analysis of gyrA mutation at position 74. Antimicrob Agents Chemother. 2011;55:608-14 pubmed publisher
    ..effect of the Ala74Ser mutant was verified through the study of the DNA supercoiling inhibitory activity of fluoroquinolones against the recombinant gyrase...
  20. Etminan M, Forooghian F, Brophy J, Bird S, Maberley D. Oral fluoroquinolones and the risk of retinal detachment. JAMA. 2012;307:1414-9 pubmed publisher
    b>Fluoroquinolones are commonly prescribed classes of antibiotics. Despite numerous case reports of ocular toxicity, a pharmacoepidemiological study of their ocular safety, particularly retinal detachment, has not been performed...