ArticleAntimicrobial agents and chemotherapy1999
Gatifloxacin activity against quinolone-resistant gyrase: allele-specific enhancement of bacteriostatic and bactericidal activities by the C-8-methoxy group.
Article in Antimicrobial agents and chemotherapy, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 91 citations in OpenAlex.
- Trial
- Gatifloxacin versus ofloxacin for the treatment of uncomplicated enteric fever in Nepal: an open-label, randomized, controlled trial.PLoS neglected tropical diseases · 2013Trial
- Gatifloxacin versus chloramphenicol for uncomplicated enteric fever: an open-label, randomised, controlled trial.The Lancet. Infectious diseases · 2011Trial
- Trial
- An open randomized comparison of gatifloxacin versus cefixime for the treatment of uncomplicated enteric fever.PloS one · 2007Trial
- A Comprehensive Review on Discovery, Development, the Chemistry of Quinolones, and Their Antimicrobial Resistance.Current topics in medicinal chemistry · 2026Review
- Investigation of bacterial DNA gyrase Inhibitor classification models and structural requirements utilizing multiple machine learning methods.Molecular diversity · 2024Article
- Article
- Clinical implications of reduced susceptibility to fluoroquinolones in paediatric Shigella sonnei and Shigella flexneri infections.The Journal of antimicrobial chemotherapy · 2016Article
- Fluoroquinolone-gyrase-DNA complexes: two modes of drug binding.The Journal of biological chemistry · 2014Article
- Specific patterns of gyrA mutations determine the resistance difference to ciprofloxacin and levofloxacin in Klebsiella pneumoniae and Escherichia coli.BMC infectious diseases · 2013Article
- Novel Conserved Genotypes Correspond to Antibiotic Resistance Phenotypes of E. coli Clinical Isolates.PloS one · 2013Article
- Fluoroquinolone and quinazolinedione activities against wild-type and gyrase mutant strains of Mycobacterium smegmatis.Antimicrobial agents and chemotherapy · 2011Article
- Molecular characterization of fluoroquinolone resistance in Mycobacterium tuberculosis: functional analysis of gyrA mutation at position 74.Antimicrobial agents and chemotherapy · 2011Article
- Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.Antimicrobial agents and chemotherapy · 2010Article
- Novel approach for comparing the abilities of quinolones to restrict the emergence of resistant mutants during quinolone exposure.Antimicrobial agents and chemotherapy · 2010Article
- Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.Antimicrobial agents and chemotherapy · 2009Article
- Use of gyrase resistance mutants to guide selection of 8-methoxy-quinazoline-2,4-diones.Antimicrobial agents and chemotherapy · 2008Article
- In vitro activity of fluoroquinolones against clinical isolates of Nocardia identified by partial 16S rRNA sequencing.European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology · 2008Article
- Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.Antimicrobial agents and chemotherapy · 2007Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Antibacterial activities of gatifloxacin (AM1155), a new C-8-methoxy fluoroquinolone, and two structurally related compounds, AM1121 and ciprofloxacin, were studied with an isogenic set of ten quinolone-resistant, gyrA (gyrase) mutants of Escherichia coli. To compare the effect of each mutation on resistance, the mutant responses were normalized to those of wild-type cells. Alleles exhibiting the most resistance to growth inhibition mapped in alpha-helix 4, which is thought to lie on a GyrA dimer surface that interacts with DNA. The C-8-methoxy group lowered the resistance due to these mutations more than it lowered resistance arising from several gyrA alleles located outside alpha-helix 4. These data are consistent with alpha-helix 4 being a distinct portion of the quinolone-binding site of GyrA. A helix change to proline behaved more like nonhelix alleles, indicating that helix perturbation differs from the other changes at helix residues. Addition of a parC (topoisomerase IV) resistance allele revealed that the C-8-methoxy group also facilitated attack of topoisomerase IV. When lethal effects were measured at a constant multiple of the minimum inhibitory concentration for each fluoroquinolone to normalize for differences in bacteriostatic action, gatifloxacin was more potent than the C-8-H compounds, both in the presence and absence of protein synthesis (an exception was observed when alanine was substituted for aspartic acid at position 82). Collectively, these data show that the C-8-methoxy group contributes to the enhanced activity of gatifloxacin against resistant gyrase and wild-type topoisomerase IV.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.