Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.4-Quinolones: QUINOLONES containing a 4-oxo (a carbonyl in the para position to the nitrogen). They inhibit the A subunit of DNA GYRASE and are used as antimicrobials. Second generation 4-quinolones are also substituted with a 1-piperazinyl group at the 7-position and a fluorine at the 6-position.Anti-Infective Agents: Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection.Fluoroquinolones: A group of QUINOLONES with at least one fluorine atom and a piperazinyl group.Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.NaphthyridinesOfloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.Microbial Sensitivity Tests: Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.Topoisomerase II Inhibitors: Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II.DNA Gyrase: A bacterial DNA topoisomerase II that catalyzes ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. Gyrase binds to DNA as a heterotetramer consisting of two A and two B subunits. In the presence of ATP, gyrase is able to convert the relaxed circular DNA duplex into a superhelix. In the absence of ATP, supercoiled DNA is relaxed by DNA gyrase.DNA Topoisomerase IV: A bacterial DNA topoisomerase II that catalyzes ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. Topoisomerase IV binds to DNA as a heterotetramer consisting 2 parC and 2 parE subunits. Topoisomerase IV is a decatenating enzyme that resolves interlinked daughter chromosomes following DNA replication.Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.QuinolinesAnti-Bacterial Agents: Substances that reduce the growth or reproduction of BACTERIA.Nalidixic Acid: A synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA GYRASE.Levofloxacin: The L-isomer of Ofloxacin.Drug Resistance, Microbial: The ability of microorganisms, especially bacteria, to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).DNA Topoisomerases, Type II: DNA TOPOISOMERASES that catalyze ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. These enzymes bring about relaxation of the supercoiled DNA and resolution of a knotted circular DNA duplex.Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.Aza CompoundsDrug Resistance, Bacterial: The ability of bacteria to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.DNA, Superhelical: Circular duplex DNA isolated from viruses, bacteria and mitochondria in supercoiled or supertwisted form. This superhelical DNA is endowed with free energy. During transcription, the magnitude of RNA initiation is proportional to the DNA superhelicity.Oxolinic Acid: Synthetic antimicrobial related to NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.Escherichia coli: A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.Staphylococcus aureus: Potentially pathogenic bacteria found in nasal membranes, skin, hair follicles, and perineum of warm-blooded animals. They may cause a wide range of infections and intoxications.Dermatitis, Phototoxic: A nonimmunologic, chemically induced type of photosensitivity producing a sometimes vesiculating dermatitis. It results in hyperpigmentation and desquamation of the light-exposed areas of the skin.Streptococcus pneumoniae: A gram-positive organism found in the upper respiratory tract, inflammatory exudates, and various body fluids of normal and/or diseased humans and, rarely, domestic animals.Gram-Positive Bacteria: Bacteria which retain the crystal violet stain when treated by Gram's method.Drug Resistance, Multiple, Bacterial: The ability of bacteria to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).Macrolides: A group of often glycosylated macrocyclic compounds formed by chain extension of multiple PROPIONATES cyclized into a large (typically 12, 14, or 16)-membered lactone. Macrolides belong to the POLYKETIDES class of natural products, and many members exhibit ANTIBIOTIC properties.Gram-Negative Bacteria: Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method.Bacteria, AnaerobicOxazines: Six-membered heterocycles containing an oxygen and a nitrogen.Bacteria: One of the three domains of life (the others being Eukarya and ARCHAEA), also called Eubacteria. They are unicellular prokaryotic microorganisms which generally possess rigid cell walls, multiply by cell division, and exhibit three principal forms: round or coccal, rodlike or bacillary, and spiral or spirochetal. Bacteria can be classified by their response to OXYGEN: aerobic, anaerobic, or facultatively anaerobic; by the mode by which they obtain their energy: chemotrophy (via chemical reaction) or PHOTOTROPHY (via light reaction); for chemotrophs by their source of chemical energy: CHEMOLITHOTROPHY (from inorganic compounds) or chemoorganotrophy (from organic compounds); and by their source for CARBON; NITROGEN; etc.; HETEROTROPHY (from organic sources) or AUTOTROPHY (from CARBON DIOXIDE). They can also be classified by whether or not they stain (based on the structure of their CELL WALLS) with CRYSTAL VIOLET dye: gram-negative or gram-positive.Clopidol: A very effective anticoccidial agent used in poultry.DNA, Bacterial: Deoxyribonucleic acid that makes up the genetic material of bacteria.Bacterial Infections: Infections by bacteria, general or unspecified.Novobiocin: An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189)Pseudomonas aeruginosa: A species of gram-negative, aerobic, rod-shaped bacteria commonly isolated from clinical specimens (wound, burn, and urinary tract infections). It is also found widely distributed in soil and water. P. aeruginosa is a major agent of nosocomial infection.Mutation: Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.Bartonella bacilliformis: The type species of the genus BARTONELLA, a gram-negative bacteria found in humans. It is found in the mountain valleys of Peru, Ecuador, and Southwest Columbia where the sandfly (see PHLEBOTOMUS) vector is present. It causes OROYA FEVER and VERRUGA PERUANA.Evodia: A plant genus of the family RUTACEAE which is used in Chinese medicine (DRUGS, CHINESE HERBAL). Evodiamine and other quinazoline alkaloids (QUINAZOLINES) are obtained from the fruit of E. ruticarpa.Mycobacterium fortuitum: A rapid-growing, nonphotochromogenic species that is potentially pathogenic, producing lesions of lung, bone, or soft tissue following trauma. It has been found in soil and in injection sites of humans, cattle, and cold-blooded animals. (Dorland, 28th ed)Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Drug Resistance, Multiple: Simultaneous resistance to several structurally and functionally distinct drugs.Tetracyclines: Closely congeneric derivatives of the polycyclic naphthacenecarboxamide. (Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1117)Genes, Bacterial: The functional hereditary units of BACTERIA.Ornidazole: A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.Aminoglycosides: Glycosylated compounds in which there is an amino substituent on the glycoside. Some of them are clinically important ANTIBIOTICS.Cephalosporins: A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid.Neisseria gonorrhoeae: A species of gram-negative, aerobic bacteria primarily found in purulent venereal discharges. It is the causative agent of GONORRHEA.Topoisomerase Inhibitors: Compounds that inhibit the activity of DNA TOPOISOMERASES.Bacterial Proteins: Proteins found in any species of bacterium.Gram-Negative Bacterial Infections: Infections caused by bacteria that show up as pink (negative) when treated by the gram-staining method.beta-Lactams: Four-membered cyclic AMIDES, best known for the PENICILLINS based on a bicyclo-thiazolidine, as well as the CEPHALOSPORINS based on a bicyclo-thiazine, and including monocyclic MONOBACTAMS. The BETA-LACTAMASES hydrolyze the beta lactam ring, accounting for BETA-LACTAM RESISTANCE of infective bacteria.Bacteria, AerobicTrimethoprim-Sulfamethoxazole Combination: This drug combination has proved to be an effective therapeutic agent with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.Quinazolinones: Chemicals with two conjoined aromatic rings incorporating two nitrogen atoms and one of the carbons oxidized with a keto oxygen.Plasmids: Extrachromosomal, usually CIRCULAR DNA molecules that are self-replicating and transferable from one organism to another. They are found in a variety of bacterial, archaeal, fungal, algal, and plant species. They are used in GENETIC ENGINEERING as CLONING VECTORS.Chloramphenicol: An antibiotic first isolated from cultures of Streptomyces venequelae in 1947 but now produced synthetically. It has a relatively simple structure and was the first broad-spectrum antibiotic to be discovered. It acts by interfering with bacterial protein synthesis and is mainly bacteriostatic. (From Martindale, The Extra Pharmacopoeia, 29th ed, p106)QuinolizinesBronchitis, Chronic: A subcategory of CHRONIC OBSTRUCTIVE PULMONARY DISEASE. The disease is characterized by hypersecretion of mucus accompanied by a chronic (more than 3 months in 2 consecutive years) productive cough. Infectious agents are a major cause of chronic bronchitis.Lactams: Cyclic AMIDES formed from aminocarboxylic acids by the elimination of water. Lactims are the enol forms of lactams.Bacteroides fragilis: Gram-negative bacteria occurring in the lower intestinal tracts of man and other animals. It is the most common species of anaerobic bacteria isolated from human soft tissue infections.Enterobacteriaceae: A family of gram-negative, facultatively anaerobic, rod-shaped bacteria that do not form endospores. Its organisms are distributed worldwide with some being saprophytes and others being plant and animal parasites. Many species are of considerable economic importance due to their pathogenic effects on agriculture and livestock.SOS Response (Genetics): An error-prone mechanism or set of functions for repairing damaged microbial DNA. SOS functions (a concept reputedly derived from the SOS of the international distress signal) are involved in DNA repair and mutagenesis, in cell division inhibition, in recovery of normal physiological conditions after DNA repair, and possibly in cell death when DNA damage is extensive.Mycobacterium avium Complex: A complex that includes several strains of M. avium. M. intracellulare is not easily distinguished from M. avium and therefore is included in the complex. These organisms are most frequently found in pulmonary secretions from persons with a tuberculous-like mycobacteriosis. Strains of this complex have also been associated with childhood lymphadenitis and AIDS; M. avium alone causes tuberculosis in a variety of birds and other animals, including pigs.Escherichia coli Infections: Infections with bacteria of the species ESCHERICHIA COLI.Ureaplasma: A genus of gram-negative, nonmotile bacteria which are common parasitic inhabitants of the urogenital tracts of humans, cattle, dogs, and monkeys.Imipenem: Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.Stenotrophomonas maltophilia: A species of STENOTROPHOMONAS, formerly called Xanthomonas maltophilia, which reduces nitrate. It is a cause of hospital-acquired ocular and lung infections, especially in those patients with cystic fibrosis and those who are immunosuppressed.Colony Count, Microbial: Enumeration by direct count of viable, isolated bacterial, archaeal, or fungal CELLS or SPORES capable of growth on solid CULTURE MEDIA. The method is used routinely by environmental microbiologists for quantifying organisms in AIR; FOOD; and WATER; by clinicians for measuring patients' microbial load; and in antimicrobial drug testing.Penicillin Resistance: Nonsusceptibility of an organism to the action of penicillins.Klebsiella pneumoniae: Gram-negative, non-motile, capsulated, gas-producing rods found widely in nature and associated with urinary and respiratory infections in humans.Drug Utilization: The utilization of drugs as reported in individual hospital studies, FDA studies, marketing, or consumption, etc. This includes drug stockpiling, and patient drug profiles.Bacterial Outer Membrane Proteins: Proteins isolated from the outer membrane of Gram-negative bacteria.Mycobacterium: A genus of gram-positive, aerobic bacteria. Most species are free-living in soil and water, but the major habitat for some is the diseased tissue of warm-blooded hosts.Spiro Compounds: A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.Viridans Streptococci: A large heterogeneous group of mostly alpha-hemolytic streptococci. They colonize the respiratory tract at birth and generally have a low degree of pathogenicity. This group of species includes STREPTOCOCCUS MITIS; STREPTOCOCCUS MUTANS; STREPTOCOCCUS ORALIS; STREPTOCOCCUS SANGUIS; STREPTOCOCCUS SOBRINUS; and the STREPTOCOCCUS MILLERI GROUP. The latter are often beta-hemolytic and commonly produce invasive pyogenic infections including brain and abdominal abscesses.Enterobacter cloacae: A species of gram-negative, facultatively anaerobic, rod-shaped bacteria that occurs in water, sewage, soil, meat, hospital environments, and on the skin and in the intestinal tract of man and animals as a commensal.Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.Urinary Tract Infections: Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.beta-Lactamases: Enzymes found in many bacteria which catalyze the hydrolysis of the amide bond in the beta-lactam ring. Well known antibiotics destroyed by these enzymes are penicillins and cephalosporins.Salmonella paratyphi A: A serotype of SALMONELLA ENTERICA that causes mild PARATYPHOID FEVER in humans.Citrobacter: A genus of gram-negative, rod-shaped enterobacteria that can use citrate as the sole source of carbon.Enterobacteriaceae Infections: Infections with bacteria of the family ENTEROBACTERIACEAE.Skin Diseases, Infectious: Skin diseases caused by bacteria, fungi, parasites, or viruses.Cilastatin: A renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.Mycoplasma pneumoniae: Short filamentous organism of the genus Mycoplasma, which binds firmly to the cells of the respiratory epithelium. It is one of the etiologic agents of non-viral primary atypical pneumonia in man.
In vitro activities of cephalosporins and quinolones against Escherichia coli strains isolated from diarrheic dairy calves. (1/269)
The in vitro activities of several cephalosporins and quinolones against 195 strains of Escherichia coli isolated from diary calves affected by neonatal diarrhea were determined. One hundred thirty-seven of these strains produced one or more potential virulence factors (F5, F41, F17, cytotoxic necrotizing factor, verotoxin, and the eae gene), but the remaining 58 strains did not produce any of these factors. From 11 to 18% of the E. coli strains were resistant to cephalothin, nalidixic acid, enoxacin, and enrofloxacin. However, cefuroxime, cefotaxime, and cefquinome were highly effective against the E. coli isolates tested. Some significant differences (P < 0.05) in resistance to quinolones between the strains producing potential virulence factors and nonfimbriated, nontoxigenic, eae-negative strains were found. Thus, eae-positive, necrotoxigenic, and verotoxigenic (except for nalidixic acid) E. coli strains were significantly more sensitive to nalidixic acid, enoxacin, and enrofloxacin than nonfimbriated, nontoxigenic, eae-negative strains. Moreover, eae-positive strains were significantly more sensitive to enoxacin and enrofloxacin than F5-positive strains. Thus, the result of this study suggest that the bovine E. coli strains that produce some potential virulence factors are more sensitive to quinolones than those that do not express these factors. (+info)Cloning, expression, and enzymatic characterization of Pseudomonas aeruginosa topoisomerase IV. (2/269)
The topoisomerase IV subunit A gene, parC homolog, has been cloned and sequenced from Pseudomonas aeruginosa PAO1, with cDNA encoding the N-terminal region of Escherichia coli parC used as a probe. The homolog and its upstream gene were presumed to be parC and parE through sequence homology with the parC and parE genes of other organisms. The deduced amino acid sequence of ParC and ParE showed 33 and 32% identity with that of the P. aeruginosa DNA gyrase subunits, GyrA and GyrB, respectively, and 69 and 75% identity with that of E. coli ParC and ParE, respectively. The putative ParC and ParE proteins were overexpressed and separately purified by use of a fusion system with a maltose-binding protein, and their enzymatic properties were examined. The reconstituted enzyme had ATP-dependent decatenation activity, which is the main catalytic activity of bacterial topoisomerase IV, and relaxing activities but had no supercoiling activity. So, the cloned genes were identified as P. aeruginosa topoisomerase IV genes. The inhibitory effects of quinolones on the activities of topoisomerase IV and DNA gyrase were compared. The 50% inhibitory concentrations of quinolones for the decatenation activity of topoisomerase IV were from five to eight times higher than those for the supercoiling activities of P. aeruginosa DNA gyrase. These results confirmed that topoisomerase IV is less sensitive to fluoroquinolones than is DNA gyrase and may be a secondary target of new quinolones in wild-type P. aeruginosa. (+info)Impact of gyrA and parC mutations on quinolone resistance, doubling time, and supercoiling degree of Escherichia coli. (3/269)
Isogenic mutants derived from quinolone-susceptible isolate WT by introducing gyrA (S83L, D87G) and parC (S80I, E84K) mutations associated with quinolone resistance were characterized with respect to quinolone resistance, growth rate, and degree of global supercoiling. The latter was determined by use of a pair of reporter plasmids carrying supercoiling-dependent promoters pgyrA and ptopA, respectively, transcriptionally fused to the reporter gene bla coding for TEM-1 beta-lactamase. The quotient (Qsc) of the beta-lactamase specific activity determined for a mutant carrying either plasmid was taken as a measure of the degree of global supercoiling. These Qsc data were comparable to results obtained from the separation of topoisomers of plasmid pBR322 on chloroquine-containing agarose gels and indicate a reduced degree of negative supercoiling in resistant mutants relative to the parent, WT. The S83L mutation in gyrA had the strongest influence on quinolone resistance while leaving other parameters nearly unaffected. The gyrA double mutation (S83L plus D87G) had an effect on quinolone resistance similar to that of a single mutation. Phenotypic expression of the parC mutation (S80I) was dependent on the presence of at least one gyrA mutation. Expression of high-level fluoroquinolone resistance (ciprofloxacin MIC, > 4 micrograms/ml) required a combination of the gyrA double mutation and one parC mutation (S80I or E84K). Such mutants showed considerable alterations of growth rate, global supercoiling, or both. Introduction of a parC mutation affected neither the doubling time nor the degree of supercoiling, while the presence of the gyrA D87G mutation was associated with a significant reduction in the degree of DNA supercoiling. (+info)Penetration of moxifloxacin into peripheral compartments in humans. (4/269)
To characterize the penetration of moxifloxacin (BAY 12-8039) into peripheral target sites, the present study aimed at measuring unbound moxifloxacin concentrations in the interstitial space fluid by means of microdialysis, an innovative clinical sampling technique. In addition, moxifloxacin concentrations were measured in cantharides-induced skin blisters, saliva, and capillary plasma and compared to total- and free-drug concentrations in venous plasma. For this purpose, 12 healthy volunteers received moxifloxacin in an open randomized crossover fashion either as a single oral dose of 400 mg or as a single intravenous infusion of 400 mg over 60 min. An almost-complete equilibration of the free unbound plasma fraction of moxifloxacin with the interstitial space fluid was observed, with mean area under the concentration-time curve (AUC)(interstitial fluid)/AUC(total-plasma) ratios ranging from 0.38 to 0.55 and mean AUC(interstitial fluid)/AUC(free-plasma) ratios ranging from 0.81 to 0.86. The skin blister concentration/plasma concentration ratio reached values above 1.5 after 24 h, indicating a preferential penetration of moxifloxacin into inflamed lesions. The moxifloxacin concentrations in saliva and capillary blood were similar to the corresponding levels in plasma. Our data show that moxifloxacin concentrations attained in the interstitial space fluid in humans and in skin blister fluid following single doses of 400 mg exceed the values for the MIC at which 90% of isolates are inhibited for most clinically relevant bacterial strains, notably including penicillin-resistant Streptococcus pneumoniae. These findings support the use of moxifloxacin for the treatment of soft tissue and respiratory tract infections in humans. (+info)Pharmacokinetics of antibiotics in burn patients. (5/269)
Drug pharmacokinetics are significantly altered in the burned patient but the interplay of a large number of variables is involved in deciding how an individual will deal with a drug. Consequently the burn patient population shows significant inter- and intrapatient variation. In 1976 altered aminoglycoside pharmacokinetics and the need for increased dosage in burn patients was reported but, despite this early study, a review of the currently available literature shows that for many drugs there is a paucity of information to support current dosage recommendations. In addition, many reports are based upon small numbers of patients, and even in larger studies there is no standardization of the study population with regard to the important variables known to affect drug handling. For the sub-population of burn patients who eliminate drugs extremely rapidly, a concern exists over the adequacy of antibiotic dosing. It is suggested that antibiotic serum concentrations be measured for all drugs in every patient to ascertain whether there is a significant problem with dosing. Additionally, future pharmacokinetic studies need to be standardized in burn patients. (+info)Activity of moxifloxacin against mycobacteria. (6/269)
Moxifloxacin is an 8-methoxyquinolone compound with activity against a wide range of bacteria. We tested its activity in comparison with four other quinolones and isoniazid against clinical isolates of mycobacteria. It proved to be the most active of the quinolones tested against Mycobacterium tuberculosis (MIC90 0.25 mg/L), Mycobacterium avium-intracellulare (MIC90 1.0 mg/L), Mycobacterium kansasii (MIC90 0.06 mg/L) and Mycobacterium fortuitum (MIC90 1 mg/L). These data indicate that moxifloxacin merits further study as an antimycobacterial agent. (+info)Characterization of MexT, the regulator of the MexE-MexF-OprN multidrug efflux system of Pseudomonas aeruginosa. (7/269)
We investigated the regulation of the MexEF-OprN multidrug efflux system of Pseudomonas aeruginosa, which is overexpressed in nfxC-type mutants and confers resistance to quinolones, chloramphenicol and trimethoprim. Sequencing of the DNA region upstream of the mexEF-oprN operon revealed the presence of an open reading frame (ORF) of 304 amino acids encoding a LysR-type transcriptional activator, termed MexT. By using T7-polymerase, a 34-kDa protein was expressed in Escherichia coli from a plasmid carrying the mexT gene. Expression of a mexE::lacZ fusion was 10-fold higher in nfxC-type mutants than in the wild-type strain; however, transcription of mexT as well as the mexT DNA region was unchanged. Located adjacent to mexT but transcribed in opposite direction, the beginning of an ORF termed qrh (quinone oxidoreductase homologue) was identified. Expression of a qrh::lacZ fusion was also found to be activated by MexT. Further, we present evidence for coregulation at the transcriptional and the posttranscriptional level between the MexEF-OprN efflux system and the OprD porin responsible for cross-resistance of nfxC-type mutants to carbapenem antibiotics. (+info)Purification and inhibition by quinolones of DNA gyrases from Mycobacterium avium, Mycobacterium smegmatis and Mycobacterium fortuitum bv. peregrinum. (8/269)
The DNA gyrases from Mycobacterium avium, Mycobacterium smegmatis and Mycobacterium fortuitum bv. peregrinum, which are species naturally resistant, moderately susceptible and susceptible to fluoroquinolones, respectively, were purified by affinity chromatography on novobiocin-Sepharose columns. The DNA gyrase inhibiting activities (IC50 values) of classical quinolones and fluoroquinolones were determined from the purified enzymes and were compared to the corresponding antibacterial activities (MICs). Regarding M. fortuitum bv. peregrinum, which is nearly as susceptible as Escherichia coli, the corresponding MIC and IC50 values of quinolones were significantly lower than those found for M. avium and M. smegmatis (e.g. for ofloxacin, MICs of 0.25 versus 32 and 1 microg ml(-1), and IC50 values of 1 versus 8 and 6 microg ml(-1), respectively). Such a result could be related to the presence of Ser-83 in the quinolone-resistance-determining region of the gyrase A subunit of M. fortuitum bv. peregrinum, as found in wild-type E. coli, instead of Ala-83 in M. avium and M. smegmatis, as found in fluoroquinolone-resistant E. coli mutants. The IC50 values of quinolones against the M. avium and M. smegmatis DNA gyrases were similar, while the corresponding MICs were 32-fold higher for M. avium when compared to M. smegmatis, suggesting that an additional mechanism, such as a low cell wall permeability or a drug efflux, could contribute to the low antibacterial potency of quinolones against M. avium. (+info)Committee on Safety of Medicines; Medicines and Healthcare products Regulatory Agency (2008). "Quinolones". United Kingdom: ... 49 (4): 468-76. doi:10.1038/clpt.1991.55. PMID 2015735. Saxon, L.; Hjemdahl, P.; Hiltunen, A. J.; Borg, S. (1997). "Effects of ... 19: 11-4. doi:10.1016/0143-4179(91)90077-V. PMID 1679209. L. Saxon, S. Borg & A. J. Hiltunen (August 2010). "Reduction of ... 12 (4): 1501-8. doi:10.1046/j.1460-9568.2000.00036.x. PMID 10762378. Rickels, Karl; Schweizer, E; Csanalosi, I; Case, WG; Chung ...
Some quinolones exert an inhibitory effect on the cytochrome P-450 system, thereby reducing theophylline clearance and ... Quinolones, including norfloxacin, may enhance the effects of oral anticoagulants, including warfarin or its derivatives or ... "Quinolones for uncomplicated acute cystitis in women". Cochrane Database Syst Rev. 3 (3): CD003597. doi:10.1002/14651858. ... The toxicity of drugs that are metabolised by the cytochrome P450 system is enhanced by concomitant use of some quinolones. ...
Allergy to quinolones Eight cases of quinolone allergy F. F. Arboit 1 , JC Bessot 2 , F. Arboit 1, JC Bessot 2, F. De Blay 2 , ... Although quinolones are highly toxic to mammalian cells in culture, its mechanism of cytotoxic action is not known. Quinolone ... Flumequine is the first quinolone compound with a fluorine atom at the C6-position of the related quinolone basic molecular ... Significant and harmful residues of quinolones have been found in animals treated with quinolones and later slaughtered and ...
... is a quinolone antibiotic used to treat bacterial infections. Pefloxacin has not been approved for use in the United ... Casparian JM, Luchi M, Moffat RE, Hinthorn D (May 2000). "Quinolones and tendon ruptures". South. Med. J. 93 (5): 488-91. doi: ... and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377-92. PMC 232616 . PMID 9293187. Khaliq Y, Zhanel GG (October 2005). " ... 32 (4): 495-502, vi. doi:10.1016/j.cps.2005.05.004. PMID 16139623. ...
Quinolones Alksne, L. (Feb 2003). "Balofloxacin Choongwae". Curr Opin Investig Drugs. 4 (2): 224-9. PMID 12669387. ...
Appelbaum, PC (1999). "Quinolone activity against anaerobes". Drugs. 58 Suppl 2: 60-4. PMID 10553708. Retrieved 13 September ... Nord, C. E. (1999). "Use of newer quinolones for the treatment of intraabdominal infections: Focus on clinafloxacin". Infection ... Rubinstein, E. (2001). "History of quinolones and their side effects". Chemotherapy. 47 Suppl 3: 3-8; discussion 44-8. doi: ...
Commonly referred to as the first generation quinolones. This first generation also included other quinolone drugs such as ... Cinoxacin is a quinolone antibiotic that has been discontinued in the U.K. as well the United States, both as a branded drug or ... Demonstration of quinolone phototoxicity in vitro. Przybilla B, Georgii A, Bergner T, Ring J. Drug Intell Clin Pharm. 1982 Dec; ... Cinoxacin was an older synthetic antimicrobial related to the quinolone class of antibiotics with activity similar to oxolinic ...
Peterson, U. (2006). "Quinolone Antibiotics: The Development of Moxifloxacin". In IUPAC; Fischer, J.; Ganellin, C. R. Analogue- ... any member of the quinolone class of antimicrobial agents, or any of the product components." Though not stated as such within ... Drlica K, Zhao X (1 September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377- ... 4% of an oral dose is excreted as either unchanged drug or known metabolites. The mean (± SD) apparent total body clearance and ...
quinolones for community-acquired pneumonia: meta-analysis of randomized controlled trials". Clin. Microbiol. Infect. 19 (4): ... Research and Development of Quinolones in Daiichi Sankyo Co., Ltd. Archived 2016-10-12 at the Wayback Machine. Page accessed ... Simultaneous use of corticosteroids is present in almost one-third of quinolone-associated tendon rupture. Tendon damage may ... Jones SF, Smith RH (March 1997). "Quinolones may induce hepatitis". BMJ. 314 (7084): 869. doi:10.1136/bmj.314.7084.869. PMC ...
Like all quinolones, it functions by inhibiting the DNA gyrase and topoisomerase IV. Topoisomerase IV is necessary to separate ... Research and Development of Quinolones in Daiichi Sankyo Co., Ltd. Archived 12 October 2016 at the Wayback Machine. Page ... Lafredo SC, Foleno BD, Fu KP (1993). "Induction of resistance of Streptococcus pneumoniae to quinolones in vitro". Chemotherapy ... Levofloxacin is the levo isomer of the racemate ofloxacin, another quinolone antimicrobial agent. Levofloxacin, a chiral ...
Ruiz, Joaquim; Pons, Maria J.; Gomes, Cláudia (September 2012). "Transferable mechanisms of quinolone resistance". ... 55 (4): 301-11. doi:10.1007/s11427-012-4310-2. PMID 22566086. Wolfe, Kenneth H.; Shields, Denis C. (Jun 12, 1997). "Molecular ... 4 (2): e4603. Bibcode:2009PLoSO...4.4603X. doi:10.1371/journal.pone.0004603. PMC 2643483 . PMID 19240804. Knowles, DG; ... 72 (4): 387-98. PMID 11826475. Rosengarten, Renate; Citti, Christine; Glew, Michelle; Lischewski, Axel; Droeße, Martina; Much, ...
Ball, P. (2000). "Quinolone generations: Natural history or natural selection?". Journal of Antimicrobial Chemotherapy. 46: 17- ... Numerous pathogens, including enterococci, Streptococcus pyogenes and Klebsiella pneumoniae (quinolone-resistant) now exhibit ... Among the 46,766 quinolone users in the study, 38 (0.1%) cases of Achilles tendon rupture were identified. A study performed ... Ciprofloxacin is the most widely used of the second-generation quinolones.[71][72] In 2010, over 20 million prescriptions were ...
Quinolone resistance genes are frequently located on the same plasmid as the ESBL genes. Examples of resistance mechanisms ... Strahilevitz J, Jacoby GA, Hooper DC, Robicsek A (October 2009). "Plasmid-mediated quinolone resistance: a multifaceted threat ... Nordmann P, Poirel L (September 2005). "Emergence of plasmid-mediated resistance to quinolones in Enterobacteriaceae". J. ... 5 (4): 113-22. PMID 12921226. Retrieved 2010-09-13. Bennett, P M (2008-03-01). "Plasmid encoded antibiotic resistance: ...
Quinolones are effective if the organism is sensitive, but high rates of quinolone use in livestock means that quinolones are ... Fàbrega A, Sánchez-Céspedes J, Soto S, Vila J (2008). "Quinolone resistance in the food chain". Int J Antimicrob Agents. 31 (4 ... 4 (9): e1000203. doi:10.1371/journal.pgen.1000203. "Campylobacter". Health Topics A TO Z. Retrieved 2011-03-06. Sherris Ternhag ...
As quinolones are known to induce arthropathy in juvenile animals, administration of the drug to breast-feeding women cannot be ... Fleroxacin is a quinolone antibiotic. It is sold under the brand names Quinodis and Megalocin. Fleroxacin is a bactericidal ... Like other quinolones and fluoroquinolones the compound eradicates bacteria by interfering with DNA replication (bacterial DNA ... Yoshida H, Nakamura M, Bogaki M, Ito H, Kojima T, Hattori H, Nakamura S (April 1993). "Mechanism of action of quinolones ...
The quinolone is also active against Gram-negative bacteria After oral administration enoxacin is rapidly and well absorbed ... "Quinolones for uncomplicated acute cystitis in women". Cochrane Database Syst Rev. 3 (3): CD003597. doi:10.1002/14651858. ... De Sarro A, Zappalá M, Chimirri A, Grasso S, De Sarro GB (July 1993). "Quinolones potentiate cefazolin-induced seizures in DBA/ ... Quinolones and fluoroquinolones are bactericidal drugs, eradicating bacteria by interfering with DNA replication. Like other ...
... (COR-167) is a drug which acts as a potent and selective cannabinoid CB2 receptor agonist, based on a quinolone-3- ... August 2008). "Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of ... August 2010). "Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and ... pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands ...
Quinolones and fluoroquinolones are bactericidal drugs, eradicating bacteria by interfering with DNA replication. Quinolones ... "As with other quinolones, exposure to the sun or ultra-violet rays may cause phototoxicity reactions in patients treated with ... Quinolones inhibit the bacterial DNA gyrase or the topoisomerase IV enzyme, thereby inhibiting DNA replication and ... Quinolone Nelson JM, Chiller TM, Powers JH, Angulo FJ (2007). "Food Safety: Fluoroquinolone‐Resistant Campylobacter Species and ...
Because of the similarity of these to the reagents in the Friedlander quinolone synthesis, a benzaldehyde with an aldehyde or ... quinolones and their annulation reactions". Tetrahedron Letters. 42 (13): 2553-2555. doi:10.1016/S0040-4039(01)00231-3. CS1 ... 40 (4): 4285-4294. doi:10.1002/cber.19070400444. Hartz, pp. 376-384 Manske, R. H. (1942). "The Chemistry of Quinolines". Chem. ... 5 (4): 145-193. doi:10.1080/00304947309355565. Rosini, M.; Anontello, A.; Cavalli, A.; Bolognesi, M.; Minarini, A.; Marucci, G ...
Quinolone-Resistant Salmonella enterica Serotype Typhimurium DT104". New England Journal of Medicine. 341 (19): 1420-1425. doi: ... 40 (4): 277-283. ISSN 1052-1372. PMC 4378521. PMID 25859123.. *^ a b Marshall, Bonnie M.; Levy, Stuart B. (October 2011). "Food ... plasmid-mediated quinolone- and macrolide-resistance genes in livestock feedlots in Northern China". Springer. 22 (6932-6940): ... 14 (4): 750-756. doi:10.1093/japr/14.4.750.. *^ Doyle, M.E. 2001: Alternatives to Antibiotic Use for Growth Promotion in Animal ...
Poisons of type II topoisomerases include etoposide, novobiocin, quinolones (including ciprofloxacin), and teniposide. These ... that renders quinolones ineffective.[citation needed] Recent structural studies have led to the discovery of a compound that no ... The experimental antitumor drug m-AMSA (4'-(9'-acridinylamino)methanesulfon-m-anisidide) also inhibits type 2 topoisomerase. ...
140 (4): 403-5. doi:10.1007/s10517-005-0503-z. PMID 16671565. He, Y.; Benz, A.; Fu, T.; Wang, M.; Covey, D.F.; Zorumski, C.F.; ... 67 (4): 310-8. doi:10.1016/j.brainresbull.2005.07.004. PMID 16182939. Yarom, M.; Tang, X. W.; Wu, E.; Carlson, R. G.; Vander ... 4 (5): 759-65. doi:10.1016/0896-6273(90)90202-Q. PMID 2160838. ; (j) Majewska MD, Harrison NL, Schwartz RD, Barker JL, Paul SM ... 5 (4): 274-280. ISSN 1021-7770. PMID 9691220. Cossart R, Bernard C, Ben-Ari Y (2005). "Multiple facets of GABAergic neurons and ...
It also has activity against Neisseria gonorrhoeae including strains that are resistant to other quinolone antibiotics. ... activity against Neisseria gonorrhoeae including quinolone-resistant strains". Diagn Microbiol Infect Dis. 62 (1): 110-112. doi ... "Comparison of pharmacokinetics between new quinolone antibiotics: the zabofloxacin hydrochloride capsule and the zabofloxacin ... 27 (4): 295-307. doi:10.1081/DCT-200039708. PMID 15573468. Jones RN, Biedenbach DJ, Ambrose PG, Wikler MA (2008). "Zabofloxacin ...
The ethyl acetate extract of R. graveolens leaves yields two furanocoumarins, one quinoline alkaloid and four quinolone ... Including a New Quinolone Alkaloid". Journal of Agricultural and Food Chemistry. 51 (4): 890-896. doi:10.1021/jf0259361. PMID ... 41 (4): 232. doi:10.1111/j.1600-0536.1999.tb06145.x. PMID 10515113. Rethy, Borbala; Zupko, Istvan; Minorics, Renata; Hohmann, ... doi:10.1016/s0031-9422(02)00284-4. PMID 12409025. INIST:13994117 Ukrainian folk songs:. Oi u poli ruta, ruta (O, rue, rue in ...
20 (4): 635-7. doi:10.1016/0091-3057(84)90316-2. PMID 6728880. Pu, C; Fisher, JE; Cappon, GD; Vorhees, CV (1994). "The effects ... In 1988 the biologist G.C. Crumplin wrote, "[AFA] is less active against bacteria than are many other 4-quinolones, but studies ... Crumplin, G.C. (1988). "Aspects of Chemistry in the Development of the 4-Quinolone Antibacterial Agents". Reviews of Infectious ... 4-dihydroxyphenylacetic acid concentration in spiperone-treated rats". Journal of Pharmacy and Pharmacology. 30 (3): 197-198. ...
The increased resistance of urinary pathogens to quinolone antibiotics has been reported worldwide and might be the consequence ... 39 (4): 210-2. PMID 22752741. Retrieved 4 April 2013.. *^ a b Jagannath VA, Fedorowicz Z, Sud V, Verma AK, Hajebrahimi S (14 ... 93 (4): 290-6. PMID 26926816.. *^ a b Nicolle LE (2001). "The chronic indwelling catheter and urinary infection in long-term- ... 28 (4): 230-41. doi:10.1097/NHH.0b013e3181dc1bcb. PMID 20520263.. *^ Opperman, EA (June 2010). "Cranberry is not effective for ...
Quinolones can be used as an alternative therapeutic option, but resistance can emerge rapidly during therapy. We analyzed the ... Quinolones can be used as an alternative therapeutic option, but resistance can emerge rapidly during therapy. We analyzed the ... Quinolones can be used as an alternative therapeutic option, but resistance can emerge rapidly during therapy. We analyzed the ... Quinolones can be used as an alternative therapeutic option, but resistance can emerge rapidly during therapy. We analyzed the ...
... quinolone) isolated from Evodia rutaecarpa showed potent anti-Helicobacter pylori activity [99]. Two alkyl quinolone compounds ... Rho TC, Bae EA, Kim DH, Oh WK, Kim BY, Ahn JS, Lee HS: Anti-Helicobacter pylori activity of quinolone alkaloids from Evodiae ... quinolone, from Evodia rutaecarpa were anti-bacterial agents highly selective in vitro against H. pylori and almost non-active ... Six quinolone alkaloids (ie evocarpine, 1-methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, 1-methyl-2-[(6Z,9Z)-6.9- ...
Garenoxacin, also called as BMS 284756, a new desfluoro(6)quinolone, is a topoiso... ... CAS: 69-53-4) Ampicillin is a beta-lactam antibiotic that is part of the aminopenicillin family and is roughly equivalent to ... CAS: 34444-01-4) Cefamandole is is the formate ester cefamandole nafate, a second-generation broad-spectrum cephalosporin ... 4. Modified biopolymer-dextrin based crosslinked hydrogels: application in controlled drug delivery ...
... quinolone (4) and 1-methyl-2-undecanone-10′-4(1H)-quinolone (5); the known compounds were identified as rutaecarpine (1), ... quinolone (6). Compounds 1-5 were evaluated for their acute toxicity. ... bodinaieri (Dode) Huang ; 2-undecyl-4(1H)-quinolone ; 1-methyl-2-undecanone-10 ′ ; -4-(1H)-quinolone ... 4.Minist Sci & Technol, Adm Ctr Chinas Agenda 21, Beijing 100089, Peoples R China. ...
Biofilm formation by Stenotrophomonas maltophilia: modulation by quinolones, trimethoprim-sulfamethoxazole, and ceftazidime. ...
It and 2-quinolone are the two most important parent (meaning simplified) quinolones. 4-Quinolone exists in equilibrium with a ... The hydroxyquinolines tautomerize to the quinolones. Andriole, VT The Quinolones. Academic Press, 1989. Shi, Pengfei; Wang, ... The chemical synthesis of quinolones often involves ring-closing reactions. Such reactions often install a hydroxyl group (an - ... Lili; Chen, Kehao; Wang, Jie; Zhu, Jin (2017). "Co(III)-Catalyzed Enaminone-Directed C-H Amidation for Quinolone Synthesis". ...
... about 4-QUINOLONES. Search and download thousands of Swedish university dissertations. Full text. Free. ... Search for dissertations about: 4-Quinolones. Found 2 swedish dissertations containing the word 4-Quinolones. ... 4-Quinolones; 2-Aminoquinazolinones; Benzoxazinones; N-Acylguanidines; Type II NADH dehydrogenase; NDH-2; ...
Repair of quinolone-induced DNA damage occurs largely via recombination pathways. In many gram-negative bacteria, resistance to ... Thus, quinolone-topoisomerase biology is providing a model for understanding aspects of host-parasite interactions and ... The key event in quinolone action is reversible trapping of gyrase-DNA and topoisomerase IV-DNA complexes. Complex formation ... moderate levels of quinolone arises from mutation of the gyrase A protein and resistance to high levels of quinolone arises ...
2-Heptyl-3-hydroxy-4-quinolone, Intercellular signal compound (CAS 108985-27-9), with ,96% purity. Join researchers using our ... Quinolone signaling in the cell-to-cell communication system of Pseudomonas aeruginosa.. Proc Natl Acad Sci U S A 96:11229-34 ( ... Biotic inactivation of the Pseudomonas aeruginosa quinolone signal molecule.. Environ Microbiol 17:4352-65 (2015). Read more ( ...
... quinolone , C21H31NO2 , CID 600305 - structure, chemical names, physical and chemical properties, classification, patents, ...
A Controlled Trial of a 4-Month Quinolone-Containing Regimen for the Treatment of Pulmonary Tuberculosis. The safety and ... In order to evaluate the efficacy and safety of the 4-month test gatifloxacin-containing regimen, comparison will be made with ... A Randomised Open-Label Controlled Trial of a 4-Month Gatifloxacin-Containing Regimen Versus Standard Regimen for the Treatment ... and all HIV infected patients at WHO stage 4. ...
Buy 4-Quinolone-3-Carboxamide CB2 Ligand - CAS Number 1314230-69-7 from LGC Standards. Please login or register to view prices ...
... quinolone (PQS), a quorum-sensing (QS) signal that regulates numerous virulence genes including those involved in iron ... Biophysical analysis revealed that 2-alkyl-3-hydroxy-4-quinolones form complexes with iron(III) at physiological … ... quinolone (PQS), a quorum-sensing (QS) signal that regulates numerous virulence genes including those involved in iron ... The Pseudomonas aeruginosa 4-quinolone signal molecules HHQ and PQS play multifunctional roles in quorum sensing and iron ...
Structure of PqsD, a Pseudomonas quinolone signal biosynthetic enzyme, in complex with anthranilate ... The enzyme is involved in the biosynthesis of the Pseudomonas Quinolone Signal ... The enzyme is involved in the biosynthesis of the Pseudomonas Quinolone Signal ... quinolone and 4-hydroxy-2(1H)-quinolone. These compounds are part of the quorum-sensing systems that is based on the production ...
4. (. [. a. n. t. R. ]. o. ×. [. PrrF. ]. ). 2. ×. [. a. n. t. R. ]. o. (3) where KDR is the dissociation constant for the antR ... Two distinct pathways supply anthranilate as a precursor of the Pseudomonas quinolone signal. J Bacteriol 189:3425-3433. doi: ... These AQs include the Pseudomonas quinolone signal (PQS) and 2-heptyl-4-hydroxyquinolone (HHQ) quorum-sensing molecules, which ... Interference with Pseudomonas quinolone signal synthesis inhibits virulence factor expression by Pseudomonas aeruginosa. Proc ...
... , E. N. Shu, K. N. ... Activity in vitro of the quinolones. In: Quinolone antimicrobial agents. Edited by D. C. Hooper, J. S. Wolfson. Washington DC: ... Detection of quinolones on thin layer chromatographic plates using sigma- and pi-acceptors in 1,4-dioxane. E. N. Shu1,*, K. N. ... Detection, quinolones, thin layer chromatography, sigma- and pi-acceptors. Introduction. Sigma- and pi-acceptors are aromatic ...
The quinolone-hydroxyquinoline tautomerism in quinolone 3-esters; preserving the 4-oxoquinoline structure to retain ... The quinolone-hydroxyquinoline tautomerism in quinolone 3-esters; preserving the 4-oxoquinoline structure to retain ... The quinolone-hydroxyquinoline tautomerism in quinolone 3-esters; preserving the 4-oxoquinoline structure to retain ... The difference between the lowest energy hydroxyquinoline and quinolone forms is 27 and 38 kJ mol-1, for 5Me-HQE and 7Me-OQE, ...
Overview of Quinolones, General information, Mechanism of action, Pharmacokinetics, Classification, Therapeutic use, Adverse ... Overview of Quinolones. by Mohammed Haneef 1. General information. 1.1. Synthetic antimicrobial agents. 1.2. First quinolone ... treated by quinolones. 5.4. Respiratory tract infections. 5.4.1. treated by respiratory fluroquinolones. 5.4.1.1. gemifloxacin ... 6.1.4. rashes. 6.1.5. insomnia. 6.1.6. dizziness. 6.1.7. headache. 6.2. hypo/hyperglycemia with gatifloxacin in old people. 6.3 ...
Get Quinolones at Spectrum Chemical. SpectrumChemical.com carries a full line of fine chemicals, lab appliances and lab ... 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic Acid TCI-C2293 , 86393-33-1 , C13H9ClFO3N , TCI America ... TCI-E0762 , 84294-96-2 , C15H17FN4O3•11/2H2O , TCI America Enoxacin Sesquihydrate ... TCI-L0193 , 100986-85-4 , C18H20FN3O4•1/2H2O , TCI America Levofloxacin ...
The quinolones are a family of synthetic broad-spectrum antibiotics. The term quinolone(s) refers to potent synthetic ... Quinolones in comparison to other antibiotic classes have the highest risk of causing colonization with MRSA and Clostridium ... The first generation of the quinolones begins with the introduction of nalidixic acid in 1962 for treatment of urinary tract ... The majority of quinolones in clinical use belong to the subset of fluoroquinolones, which have a fluorine atom attached to the ...
The small RNA PhrS stimulates synthesis of the Pseudomonas aeruginosa quinolone signal. Authors. *. Elisabeth Sonnleitner,. ... 4. Matthias Gimpel, Sabine Brantl, Dual-function small regulatory RNAs in bacteria, Molecular Microbiology, 2017, 103, 3, 387. ... MMI_7620_sm_FigS1-4_TableS1-2.pdf207K. Supporting info item. ... 4, e1005975. CrossRef. *16. Lucía Fernández, Elena B. M. ...
quinolone any chemical compound having 2-quinolone or 4-quinolone skeleton in its structure ... Quinolone (en-ca); Chinoloni (it); quinolone (fr); Kinoloonid (et); Kinolon (sv); 喹诺酮 (zh-hans); quinolona (pt); Hinolon (sr-el ... quinolones (en); chinolony (pl); Kinoloner (nb); Quinolone, Quinolon, Quinolonen, Chinolonen (nl) ... Media in category "Quinolones". The following 35 files are in this category, out of 35 total. ...
... ... 7-[(3r)-3-aminopyrrolidin-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid. ...
We review macrolide and quinolone resistance in Campylobacter and track resistance trends in human clinical isolates in ... coli infections has increased markedly in many parts of the world in the last decade as has the number of quinolone-resistant ... The induction of quinolone resistance in Campylobacter in broilers by quinolone treatment. Lett Appl Microbiol. 1994; 19228-31. ... Overview of quinolone usage for food-producing animals. In: Use of quinolones in food animals and potential impact on human ...
Coli MIC of Quinolone Derivatives. In: Antimicrobial Prophylaxis in Urology with special reference to the new Quinolones. ... Chin NX, Neu HC (1983) In vitro activity of enoxacin, a quinolone carboxylic acid, compared with those of norfloxacin, new ß- ... Antimicrobial Prophylaxis in Urology with special reference to the new Quinolones pp 43-46 , Cite as ... The Influence of Various Body Fluids and pH on E. Coli MIC of Quinolone Derivatives. ...
LevofloxacinPlasmid-mediated quinolone resistance genesDevelopment of quinolone resistanceCharacterization of quinolone resistanceAntibacterial agentsCarboxylic acidEnterobacteriaceaeNorfloxacinSalmonellaPMQRExposure to quinolonesLevels of quinoloneEscherichiaMutationsSusceptibilityVitro activitySyntheticAzithromycinMacrolidesDiarrhoea1998OfloxacinInteractionsPreclinicalIntercellularGeneQuinolineConferCarbonylAnticancerSkeletonAntimicrobial ActivityRegulation
- Fifty-five levofloxacin nonsusceptible (minimum inhibitory concentration [MIC] ≥4 μg/ml) and 47 susceptible (MIC ≤2 μg/ml) isolates were tested for efflux pump overexpression. (elsevier.com)
- Prevalence of plasmid-mediated quinolone resistance genes and ciprofloxacin resistance in pediatric bloodstream isolates of Enterobacteriaceae over a 9-year period. (medworm.com)
- Besides, plasmid-mediated quinolone resistance genes also confer low levels of quinolone resistance [ 10 ]. (hindawi.com)
- More information on the prevalence of qnr in clinical strains is needed to understand its importance and contribution to the development of quinolone resistance. (asm.org)
- Cloning and nucleotide sequence of the Campylobacter jejuni gyrA gene and characterization of quinolone resistance mutations. (cdc.gov)
- Moreover, topoisomerase IV is a target of the 4-quinolones, antibacterial agents that had previously been thought to target only gyrase. (asm.org)
- Synergic effect of quinolone antibacterial agents and proton pump inhibitors on Helicobacter pylori ," Journal of Antimicrobial Chemotherapy , vol. 49, no. 6, pp. 1039-1040, 2002. (hindawi.com)
- Ciprofloxacin and ofloxacin are both 4-quinolones containing a carboxylic acid moiety in the 3 position of the basic ring structure, a fluorine substituent at position 6, and a piperazine moiety at position 7 [ 12 ]. (alliedacademies.org)
- For example, the quinolone nucleus contains a carboxylic acid group at position 3 and an exocyclic oxygen at position 4 (hence the term 4-quinolones), which are believed to be the active DNA-gyrase binding sites. (merckvetmanual.com)
- A quinolone that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted at positions 1, 6, and 7 by 2,4-difluorophenyl, fluorine, and 3-methylpiperazin-1-yl groups, respectively. (ebi.ac.uk)
- Klebsiella pneumoniae and Escherichia coli are the two most common quinolone-resistant Enterobacteriaceae . (hindawi.com)
- Norfloxacin: a new quinolone. (cmaj.ca)
- Provides information on a study that monitored resistance to the drug quinolones in Salmonella enterica serotype enteritidis from human infections. (ebscohost.com)
- Plasmid-mediated quinolone resistance (PMQR) has received considerable attention recently. (peerj.com)
- Due to the increase in fluoroquinolone resistance, plasmid-mediated quinolone resistance (PMQR) has received considerable attention in recent years. (peerj.com)
- Thus, children can be considered as a population lacking exposure to quinolones. (hindawi.com)
- In many gram-negative bacteria, resistance to moderate levels of quinolone arises from mutation of the gyrase A protein and resistance to high levels of quinolone arises from mutation of a second gyrase and/or topoisomerase IV site. (asm.org)
- We report an atypical enteropathogenic Escherichia coli O127a:K63 strain with resistance to quinolones and extended-spectrum cephalosporins isolated from a 2010 food poisoning outbreak involving 112 adults in China. (asm.org)
- Recipient(s) will receive an email with a link to 'Association of plasmid-mediated quinolone resistance and virulence markers in Escherichia coli isolated from water' and will not need an account to access the content. (iwaponline.com)
- Multiple Copies of qnrA1 on an IncA/C2 Plasmid Explain Enhanced Quinolone Resistance in an Escherichia coli Mutant. (harvard.edu)
- Quinolone resistance is usually caused by chromosomal mutations, but plasmid-mediated quinolone resistance has been discovered recently. (asm.org)
- The mutations in the quinolone resistance-determining regions in gyrA gene were detected by PCR and DNA sequencing. (hindawi.com)
- Resistance to quinolones in enterobacteria is mainly due to mutations in the quinolone target enzymes (DNA gyrase and topoisomerase IV) encoded by gyrA and parC [ 8 , 9 ]. (hindawi.com)
- 4. Drug susceptibility at the outset will be useful in such areas. (ersjournals.com)
- The present invention is directed to a lyophilized preparation which contains a synthetic quinolone antibacterial compound and, as a solo additive, a pH-adjusting agent, and which exhibits an excellent reconstituting property. (patents.com)
- The invention provides a method for producing a lyophilized preparation containing a synthetic quinolone antibacterial compound as an active ingredient, characterized by including, sequentially, cooling an aqueous solution containing a synthetic quinolone antibacterial compound and a pH-adjusting agent to yield a frozen product, elevating the temperature of the frozen product, and re-cooling the resultant to prepare the lyophilized preparation. (patents.com)
- Moreover, a retrospective analysis of patients with ABECB showed that the administration of a broader spectrum antimicrobial agent (azithromycin, quinolone or amoxicillin/clavulanate (A/C)) was associated with fewer clinical failures compared with the use of first-line agents (mainly amoxicillin, TMP/SMX, and doxycycline) 15 . (ersjournals.com)
- There was no difference regarding treatment success in intention-to-treat and clinically evaluable patients between macrolides and quinolones, A/C and quinolones or A/C and macrolides. (ersjournals.com)
- The treatment success in microbiologically evaluable patients was lower for macrolides compared with quinolones (odds ratio (OR) 0.47, 95% confidence interval (CI) 0.31-0.69). (ersjournals.com)
- Adverse effects in general were similar between macrolides and quinolones. (ersjournals.com)
- Macrolides, quinolones and A/C have been used extensively for the management of patients with ABECB. (ersjournals.com)
- The present study sought to further clarify the role of broader spectrum antimicrobial agents for the treatment of patients with ABECB by performing a meta-analysis of RCTs that compared macrolides with quinolones, A/C with quinolones or A/C with macrolides in this population. (ersjournals.com)
- Administration of A/C was associated with more adverse effects (mainly diarrhoea) than quinolones (OR 1.36, 95% CI 1.01-1.85). (ersjournals.com)
- Smith KE , Besser JM , Hedberg CW , Leano FT , Bender JB , Wicklund JH , Quinolone-resistant Campylobacter jejuni infections in Minnesota, 1992-1998. (cdc.gov)
- Background: The first report on the transferable, plasmid-mediated quinolone-resistance determinant qnrA1 was in 1998. (ebscohost.com)
- The PrrF sRNAs promote the production of 2-akyl-4(1 H )-quinolone metabolites (AQs) that mediate a range of biological activities, including quorum sensing and polymicrobial interactions. (asm.org)
- Docking studies performed in silico at the yeast Qo site established a key role for the 4-oxo and N-H groups in drug-target interactions. (unl.pt)
- Endochin-like-quinolones (ELQs) are preclinical compounds that are efficacious against apicomplexan-caused diseases including toxoplasmosis, malaria and babesiosis. (blogspot.com)
- The demonstration that 2-heptyl-3-hydroxy-4-quinolone can function as an intercellular signal sheds light on the role of secondary metabolites and shows that P. aeruginosa cell-to-cell signaling is not restricted to acyl-homoserine lactones. (pnas.org)
- Although quinolone resistance commonly results from chromosomal mutation, recent studies indicate that such resistance can also be transferred on plasmids carrying the gene responsible, qnr . (asm.org)
- Results: We conducted random and site-directed mutagenesis on qnrA1 and on qnrC, a newly identified quinolone-resistance gene from Proteus mirabilis. (ebscohost.com)
- 4-Quinolone is an organic compound derived from quinoline. (wikipedia.org)
- E ) 2-heptyl-4-hydroxy-quinoline- N -oxide. (pnas.org)
- 2-Quinolone is an organic compound related structurally to quinoline. (wikipedia.org)
- Qnr proteins confer quinolone resistance, and belong to the pentapeptide repeat protein (PRP) family. (ebscohost.com)
- QUINOLONES containing a 4-oxo (a carbonyl in the para position to the nitrogen). (bioportfolio.com)
- Voreloxin, a first-in-class anticancer quinolone derivative, acts synergistically with cytarabine in vitro and induces bone marrow aplasia in vivo. (nih.gov)
- 4. The method for producing a lyophilized preparation of claim 1, wherein X.sup.2 is a C1-C6 alkoxy group or a ring structure which contains, as a ring-constituting atom, an oxygen atom, a nitrogen atom, or a sulfur atom and which is formed from X.sup.2, R.sup.1, and a part of the quinolone skeleton. (patents.com)
- Within the diversity of their various ring structures, the quinolones have a number of common functional groups essential for their antimicrobial activity. (merckvetmanual.com)
- Subsequently, the expression of lasB also was shown to be controlled by C 4 -HSL and RhlR, indicating that both known P. aeruginosa cell-to-cell signals were involved in the regulation of this major virulence factor ( 4 , 10 - 12 ). (pnas.org)