Quinolones are a large and widely consumed class of synthetic drugs. Expanded-spectrum quinolones, like ciprofloxacin are highly effective against Gram-negative bacteria, especially Escherichia coli. In E. coli the major target for quinolones is DNA gyrase. This enzyme is composed of two subunits, GyrA and GyrB encoding by gyrA and gyrB, respectively. Mutations in either of these genes cause qu...

Methods A total of 100 ofloxacin resistant (OFX r) and 100 OFX sensitive (OFX s) isolates of M.tuberculosis isolates were consecutively selected from routine TB laboratory during 2012-2013. All the isolates were screened for phenotypic OFX r (>2μg/ml) by 1% proportion method and tested for minimal inhibitory concentration by absolute concentration method. Quinolone resistance determining region...

quinolones are a large and widely consumed class of synthetic drugs. expanded-spectrum quinolones, like ciprofloxacin are highly effective against gram-negative bacteria, especially escherichia coli. in e. coli the major target for quinolones is dna gyrase. this enzyme is composed of two subunits, gyra and gyrb encoding by gyra and gyrb, respectively. mutations in either of these genes cause qu...

  Target modification and reduced drug accumulation are the main resistance mechanisms against fluoroquinolone antibiotics in Pseudomonas aeruginosa. We performed a genotypic characterization of three major Mex multidrug efflux pumps (MexAB-OprM, MexXY-OprM and MexCD-OprJ) in ciprofloxacin resistant clinical isolates of P. aeru­ginosa, collected from Tehran, Iran this was followed by sequencin...

DNA topoisomerases manage chromosome supercoiling and organization in all forms of life. Gyrase, a prokaryotic heterotetrameric type IIA topo, introduces negative supercoils into DNA by an ATP-dependent strand passage mechanism. All gyrase orthologs rely on a homologous set of catalytic domains for function; however, these enzymes also can possess species-specific auxiliary regions. The gyrases...

Flavonoids are potential antibacterial agents. However, key substituents and mechanism for their antibacterial activity have not been fully investigated. The quantitative structure-activity relationship (QSAR) and molecular docking of flavonoids relating to potent anti-Escherichia coli agents were investigated. Comparative molecular field analysis (CoMFA) and comparative molecular similarity in...

Bacterial DNA gyrase is an important target of antibacterial agents, including fluoroquinolones. In most bacterial species, fluoroquinolones inhibit DNA gyrase and topoisomerase IV and cause bacterial cell-death. Other naturally occurring bacterial DNA gyrase inhibitors, such as novobiocin, are also known to be effective as antibacterial agents. DNA gyrase is an ATP-dependent enzyme that acts b...