Since quinine was first isolated, animals, plants and microorganisms producing a wide variety of quinolone compounds have been discovered, several of which possess medicinally interesting properties ranging from antiallergenic and anticancer to antimicrobial activities. Over the years, these have served in the development of many synthetic drugs, including the successful fluoroquinolone antibio...

novel analogues of n-piperazinyl fluoroquinolones were prepared and evaluated against a panel of gram-positive and gram-negative bacteria, to study the effect of introducing bulky anthracene and phenanthrene moieties on the antibacterial effects of norfloxacin, ciprofloxacin and gatifloxacin. although most of the novel synthesized compounds had lower antibacterial effects, some derivatives show...

The structural features of copper(II), nickel(II), cobalt(II) and zinc(II) complexes with the antimicrobial drugs quinolones and non-steroidal anti-inflammatory drugs (NSAIDs) as ligands are discussed. The binding properties of these complexes to biomolecules (calf-thymus DNA, bovine or human serum albumin) are presented and evaluated. The biological activity (antimicrobial, antioxidant and ant...

Antimicrobial resistance among human pathogens which is not related to veterinary use 6 Mechanism of (fluoro)quinolone resistance and interpretation of susceptibility tests....... 6 Selection for resistance in food borne pathogens when using (fluoro)quinolones in food-MANDATE The Scientific Advisory Group on Antimicrobials (SAGAM) was mandated to give advice to the CVMP on the need to exercise ...

Although resistance to quinolones is commonly chromosomally-encoded in Enterobacteriaceae, the emergence of plasmid-mediated quinolone resistance (PMQR) has also been reported, with at least three known resistance mechanisms to date, i.e., Qnr, aminoglycoside acetyltransferase AAC(6')-Ib-cr and QepA. Qnr proteins protect target enzymes (DNA gyrase and type IV topoisomerase) from quinolone inhib...

perazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid] (Fig. 1) is a broad spectrum fluoroquinolone antibacterial, which is effective against a wide range of Gram-positive and Gram-negative bacteria (1). Fluoroquinolones are sensitive to light (2) and studies have been carried out on the photodegradation of quinolones (3), fluoroquinolones (4), ciprofloxacin (5, 6), sparfloxaci...

The quinolones trap DNA gyrase and DNA topoisomerase IV on DNA as complexes in which the DNA is broken but constrained by protein. Early studies suggested that drug binding occurs largely along helix-4 of the GyrA (gyrase) and ParC (topoisomerase IV) proteins. However, recent X-ray crystallography shows drug intercalating between the -1 and +1 nucleotides of cut DNA, with only one end of the dr...

enoxacin and norfloxacin on inclusion development and infectivity. The MICs and MLCs of these drugs are compared in Table 1. There was considerable variation in the sensitivity of C. trachomatis to these quinolones, which may reflect their varying ability to penetrate eukaryotic cells. However, at effective concentrations, the action of each drug was lethal, i.e. infectivity was not affected by...