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.
Mutation of a conserved serine residue in a quinolone-resistant type II topoisomerase alters the enzyme-DNA and drug interactions. (1/2071)A Ser740 --> Trp mutation in yeast topoisomerase II (top2) and of the equivalent Ser83 in gyrase results in resistance to quinolones and confers hypersensitivity to etoposide (VP-16). We characterized the cleavage complexes induced by the top2(S740W) in the human c-myc gene. In addition to resistance to the fluoroquinolone CP-115,953, top2(S740W) induced novel DNA cleavage sites in the presence of VP-16, azatoxin, amsacrine, and mitoxantrone. Analysis of the VP-16 sites indicated that the changes in the cleavage pattern were reflected by alterations in base preference. C at position -2 and G at position +6 were observed for the top2(S740W) in addition to the previously reported C-1 and G+5 for the wild-type top2. The VP-16-induced top2(S740W) cleavage complexes were also more stable. The most stable sites had strong preference for C-1, whereas the most reversible sites showed no base preference at positions -1 or -2. Different patterns of DNA cleavage were also observed in the absence of drug and in the presence of calcium. These results indicate that the Ser740 --> Trp mutation alters the DNA recognition of top2, enhances its DNA binding, and markedly affects its interactions with inhibitors. Thus, residue 740 of top2 appears critical for both DNA and drug interactions. (+info)
Vasopressin V2 receptor enhances gain of baroreflex in conscious spontaneously hypertensive rats. (2/2071)The aim of the present study was to determine the receptor subtype involved in arginine vasopressin (AVP)-induced modulation of baroreflex function in spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats using novel nonpeptide AVP V1- and V2-receptor antagonists. Baroreceptor heart rate (HR) reflex was investigated in both SHR and WKY rats which were intravenously administered the selective V1- and V2-receptor antagonists OPC-21268 and OPC-31260, respectively. Baroreflex function was assessed by obtaining alternate pressor and depressor responses to phenylephrine and sodium nitroprusside, respectively, to construct baroreflex curves. In both SHR and WKY rats baroreflex activity was tested before and after intravenous administration of vehicle (20% DMSO), OPC-21268 (10 mg/kg), and OPC-31260 (1 and 10 mg/kg). Vehicle did not significantly alter basal mean arterial pressure (MAP) and HR values or baroreflex function in SHR or WKY rats. The V1-receptor antagonist had no significant effect on resting MAP or HR values or on baroreflex parameters in both groups of rats, although this dose was shown to significantly inhibit the pressor response to AVP (5 ng iv; ANOVA, P < 0.05). In SHR but not WKY rats the V2-receptor antagonist significantly attenuated the gain (or slope) of the baroreflex curve (to 73 +/- 3 and 79 +/- 7% of control for 1 and 10 mg/kg, respectively), although AVP-induced pressor responses were also attenuated with the higher dose of the V2-receptor antagonist. These findings suggest that AVP tonically enhances baroreflex function through a V2 receptor in the SHR. (+info)
Carrier-mediated lung distribution of HSR-903, a new quinolone antibacterial agent. (3/2071)HSR-903 [(S)-(-)-5-amino-7-(7-amino-5-azaspiro[2. 4]hept-5-yl)-1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid methanesulfonate] is a newly synthesized quinolone with a potent antibacterial activity and a low toxicity. The lung concentration of unchanged HSR-903 was about nine times higher than that in plasma after oral administration (5 mg/kg) in rats. In comparative studies, HSR-903 was accumulated more efficiently than levofloxacin, ciprofloxacin, and lomefloxacin in rat lung. To clarify the mechanism of the specific distribution of HSR-903 into the lung, the uptake of [14C]HSR-903 was studied using isolated rat lung cells and an isolated rat lung perfusion technique. Initial uptake of HSR-903 by isolated lung cells was temperature dependent, saturable, stereospecific, and Na+ and Cl- dependent. The Hill coefficients (1. 90 for Na+ and 1.13 for Cl-) suggest that two Na+ and one Cl- are associated with the transport of one HSR-903 molecule. The uptake of HSR-903 was inhibited by other quinolone antibacterial agents, grepafloxacin, and sparfloxacin. The extraction ratio of HSR-903 in isolated lung perfusion was temperature dependent and saturable. These findings suggest that HSR-903 is taken up by the lung cells via a carrier-mediated transport mechanism, resulting in a concentrative distribution into the lung. (+info)
Activation of a cGMP-stimulated cAMP phosphodiesterase by protein kinase C in a liver Golgi-endosomal fraction. (4/2071)The ability of Ca2+/phospholipid-dependent protein kinase (protein kinase C, PKC) to stimulate cAMP phosphodiesterase (PDE) activity in a liver Golgi-endosomal (GE) fraction was examined in vivo and in a cell-free system. Injection into rats of 4 beta-phorbol 12-myristate 13-acetate, a known activator of PKC, caused a rapid and marked increase in PKC activity (+325% at 10 min) in the GE fraction, along with an increase in the abundance of the PKC alpha-isoform as seen on Western immunoblots. Concurrently, 4 beta-phorbol 12-myristate 13-acetate treatment caused a time-dependent increase in cAMP PDE activity in the GE fraction (96% at 30 min). Addition of the catalytic subunit of protein kinase A (PKA) to GE fractions from control and 4 beta-phorbol 12-myristate 13-acetate-treated rats led to a comparable increase (130-150%) in PDE activity, suggesting that PKA is probably not involved in the in-vivo effect of 4 beta-phorbol 12-myristate 13-acetate. In contrast, addition of purified PKC increased (twofold) PDE activity in GE fractions from control rats but affected only slightly the activity in GE fractions from 4 beta-phorbol 12-myristate 13-acetate-treated rats. About 50% of the Triton-X-100-solubilized cAMP PDE activity in the GE fraction was immunoprecipitated with an anti-PDE3 antibody. On DEAE-Sephacel chromatography, three peaks of PDE were sequentially eluted: one early peak, which was stimulated by cGMP and inhibited by erythro-9 (2-hydroxy-3-nonyl) adenine (EHNA); a selective inhibitor of type 2 PDEs; and two retarded peaks of activity, which were potently inhibited by cGMP and cilostamide, an inhibitor of type 3 PDEs. Further characterization of peak I by HPLC resolved a major peak which was activated (threefold) by 5 microM cGMP and inhibited (87%) by 25 microM EHNA, and a minor peak which was insensitive to EHNA and cilostamide. 4 beta-Phorbol 12-myristate 13-acetate treatment caused a selective increase (2.5-fold) in the activity associated with DEAE-Sephacel peak I, without changing the K(m) value. These results suggest that PKC selectively activates a PDE2, cGMP-stimulated isoform in the GE fraction. (+info)
A mutation in QRDR in the ParC subunit of topoisomerase IV was responsible for fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae. (5/2071)Forty-one strains of Streptococcus pneumoniae were isolated at Seoul National University Children's Hospital from 1991 to 1997. Isolates were divided into six groups based on MICs of three quinolones, ciprofloxacin, ofloxacin and norfloxacin. Sequencing showed that the isolates which were intermediately resistant to three quinolones or resistant to at least one kind of quinolone had one missense mutation, Lys137-->Asn(AAG-->AAT) substitution in the ParC subunit of topoisomerase IV without additional mutation in QRDR of the GyrA subunit of DNA gyrase. In conclusion, the ParC subunit of DNA topoisomerase IV is the primary target site for fluoroquinolone in S. pneumoniae and Lys137-->Asn substitution renders the quinolone resistance in S. pneumoniae. (+info)
Inflammatory pseudotumor in a cat with cutaneous mycobacteriosis. (6/2071)A 5-year-old, castrated male, domestic Shorthair Cat had an ulcerated mass with fistulous tracts on the left hind paw. Homogeneous tan tissue diffusely infiltrated the dermis and subcutis of the paw and extended proximally so that, short of amputation, complete excision was not feasible. Biopsy specimens consisted of granulation tissue with marked proliferation of spindle cells. Neutrophils and histiocytic cells were scattered among the spindle cells. The histiocytic cells had abundant foamy or vacuolated cytoplasm, but features of granulomatous inflammation, such as epithelioid macrophages or granuloma formation, were not observed. The initial impression was inflammatory granulation tissue, but the degree of fibroplasia prompted inclusion of fibrosarcoma in the differential diagnosis. Cutaneous mycobacteriosis was diagnosed when numerous acid-fast bacteria were identified with Kinyoun's stain; Mycobacterium avium was subsequently cultured. The cat was euthanatized because of lack of response to enrofloxacin therapy. At necropsy, lesions were localized to the hind limb. Not only is mycobacteriosis an uncommon cause of cutaneous masses in cats, but this case was unusual because of the lack of granuloma formation and the similarity of the mass to a spindle cell tumor. (+info)
Indomethacin-induced gastric antral damage in hamsters: are neutrophils involved? (7/2071)BACKGROUND: A direct role for neutrophils in the pathophysiology of indomethacin-induced gastric damage is controversial. Therefore, such damage was evaluated in hamsters. METHODS: Gastric antral damage was evaluated 4 h after the oro-gastric administration of indomethacin (30 mg/kg). Prior to indomethacin, hamsters were treated with various pharmacological agents: rebamipide, methotrexate or anti-neutrophil serum (ANS). The number of circulating neutrophils was determined from Wright-Giemsa stained blood smears. Myeloperoxidase (MPO) activity was measured as a marker of gastric antral neutrophil infiltration. RESULTS: Indomethacin caused primarily gastric antral damage. By histology, this damage did not penetrate the muscularis mucosa. A significant increase in gastric antral MPO activity was also found in indomethacin-treated hamsters. Rebamipide decreased macroscopic gastric antral damage in a dose-related fashion. Methotrexate treatment reduced the circulating blood neutrophil number by 38-44%, but did not affect gastric damage. ANS treatment resulted in near complete neutropenia, and also in a substantial reduction (84%) in gastric antral MPO activity. However, gastric antral damage was not significantly altered by ANS. CONCLUSIONS: Neutrophils are not directly involved in the pathophysiology of indomethacin-induced damage to the hamster gastric antrum. (+info)
Pharmacodynamic effects of subinhibitory concentrations of rufloxacin on bacterial virulence factors. (8/2071)It has been reported that subinhibitory concentrations (sub-MICs) of some fluoroquinolones are still capable of affecting the topological characteristics of DNA (inhibition DNA-gyrase) and that this leads to a reduction in some of the factors responsible for bacterial virulence (by means of the disruption of protein synthesis and alterations in phenotype expression), even though the microorganisms themselves are not killed. The present study investigated the ability of sub-MICs of rufloxacin, an orally absorbed monofluorinated quinolone with a long half-life (28 to 30 h), to interfere with the bacterial virulence parameters of adhesiveness, hemagglutination, hydrophobicity, motility, and filamentation, as well as their interactions with host neutrophilic defenses such as phagocytosis, killing, and oxidative bursts. It was observed that Escherichia coli adhesiveness was significantly reduced at rufloxacin concentrations of 1/32 MIC, hemagglutination and hydrophobicity were significantly reduced at concentrations of, respectively, 1/4 MIC and 1/8 MIC, and motility was significantly reduced at concentrations of 1/16 MIC; filamentation was still present at concentrations of 1/4 MIC. Phagocytosis was not affected, but killing significantly increased from 1/2 MIC to 1/8 MIC; oxidative bursts measured by means of chemiluminescence were not affected. The fact that sub-MICs are still effective in interfering with the parameters of bacterial virulence is useful information that needs to be correlated with pharmacokinetic data in order to extend our knowledge of the most effective concentrations that can be used to optimize treatment schedules, for example, single administrations, particularly in noncomplicated lower urinary tract infections. (+info)
Plasmid-mediated quinolone resistance determinants among Gram-negative bacteraemia isolates: a hidden threat | Microbiology...
Purpose. The aim of the study was to investigate the prevalence of plasmid-mediated quinolone resistance (PMQR) genes in an unselected collection of bloodstream isolates recovered over an 18-month period in a laboratory affiliated to a university hospital in Athens, Greece, and to assess their impact on the in vitro activity of ciprofloxacin and levofloxacin. Methods. Eight PMQR genes were screened by PCR and sequencing. All PMQR-positive isolates were submitted to isoelectric focusing for β-lactamase detection, conjugation or transformation, time-kill assays, mutant prevention concentrationand inoculum effect evaluation. PCR and sequencing of gyrA and parC were performed for detection of chromosomal mutations. Results. Among 96 Gram-negative isolates, 7 (7.3 %) carried one or more PMQR genes. qnrS1 was the most prevalent (5.2 %), followed by aac(6′ )-Ib-cr (4.2 %) and their combination (2 %). Cloning was successful for three isolates. The presence of a single PMQR determinant without any target
High incidence of plasmid-mediated quinolone resistance genes among ciprofloxacin-resistant clinical isolates of...
Background. Plasmid-mediated quinolone resistance (PMQR) has received considerable attention recently. Data analysis in Jawaharlal Institute of Postgraduate Medical Education & Research (JIPMER) revealed 75% of the Enterobacteriaceae isolates to be ciprofloxacin-resistant in 2012. Few reports regarding the prevalence of PMQR are available from India. Hence, the present study was carried out to ascertain the prevalence of PMQR genes among clinical isolates of ciprofloxacin-resistant Enterobacteriaceae in JIPMER. Methods. The study included 642 ciprofloxacin-resistant clinical Enterobacteriaceae isolates. JIPMER hospitals annual consumption data for fluoroquinolones were retrieved from the Department of Pharmacy. The test isolates were screened for the presence of qnr A, B, D, S and aac(6′)-Ib-cr genes. PMQR-positive isolates alone were tested for the presence of class I (intI1) and class II (intI2) integrons. Randomly selected PCR amplicons were sequenced and analysed using MEGA software. A total of
7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic...
The effects of 7-(4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2 (1H)- quinolinone (OPC-14597), a derivative of the dopamine (DA) autoreceptor agonist 7-(3-[4-(2,3-dimethylphenyl)piperazinyl]propoxy)-2(1H)-quinolinone (OPC-4392), on DA receptors were biochemically and behaviorally studied and compared with those of OPC-4392. Both OPC-14597 and OPC-4392 inhibited reserpine- and gamma-butyrolactone (GBL)-induced increase in tyrosine hydroxylase activity in the mouse and rat brain. The effects of OPC-14597 were comparable to those of OPC-4392 and were completely antagonized by haloperidol. OPC-14597, unlike apomorphine, did not evoke postsynaptic DA receptor-stimulating behavioral signs such as hyperlocomotion in the reserpinized mice and contralateral rotation in rats with unilateral striatal 6-hydroxydopamine lesions. Both OPC-14597 and OPC-4392 inhibited such apomorphine-induced postsynaptic behavioral changes as stereotypy and hyperlocomotion in mice and rats and rotation in ...
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Broad Dissemination of Plasmid-Mediated Quinolone Resistance Genes in Sediments of Two Urban Coastal Wetlands
Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations in quinolone-resistant...
TY - JOUR. T1 - Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations in quinolone-resistant Escherichia coli isolated from humans and swine in Denmark. AU - Cavaco, Lina. AU - Frimodt-Møller, Niels. AU - Hasman, Henrik. AU - Guardabassi, Luca. AU - Nielsen, Lene. AU - Aarestrup, Frank Møller. PY - 2008. Y1 - 2008. N2 - Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations (MICs) of nalidixic acid (NAL) and ciprofloxacin (CIP) were investigated in 124 Escherichia coli isolated from humans (n = 85) and swine (n = 39) in Denmark. The collection included 59 high-level CIP-resistant isolates (MIC ,= 4) from human (n = 51) and pig origin (n = 8) and 65 low-level CIP-resistant isolates (MIC ,= 0.125) from human (n = 34) and pig origin (n = 31). Resistance by target modification was screened by PCR amplification and sequencing, of the quinolone resistance determining regions (QRDRs) of gyrA, gyrB, parC, and ...
Microbiology Society Journals | Detection of mutations in the gyrA and parC genes in Escherichia coli isolates carrying plasmid...
In this study, the prevalence of plasmid-mediated quinolone resistance (PMQR) was investigated in 495 Escherichia coli isolates from diseased food-producing animals in Guangdong province, China. The quinolone resistance-determining regions (QRDRs) of the gyrA and parC genes were analysed for mutations in 55 isolates harbouring only oqxAB and all isolates harbouring other PMQR genes. Overall, 282 (57.0 %) E. coli isolates had at least one PMQR gene. oqxAB was detected in 215 isolates and predominated the PMQR genes, followed by qnrS (63 isolates), aac(6′)-Ib-cr (56 isolates), qnrB (39 isolates) and qepA (18 isolates). qnrA, qnrC and qnrD were not found in any of the isolates. The rates of resistance to ciprofloxacin, enrofloxacin, levofloxacin and nalidixic acid were 75.2, 81.0, 70.5 and 97.4 %, respectively, among the 495 isolates. Eight types of mutation in gyrA were detected in 154 PMQR-positive isolates, and 147 isolates were found to have mutations in parC. PFGE analysis indicated that the PMQR
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"Chronic administration of aripiprazole activates GSK3β-dependent signa" by Bo Pan, Xu-Feng Huang et al.
Aripiprazole is a D2-like receptor (D2R) partial agonist with a favourable clinical profile. Previous investigations indicated that acute and short-term administration of aripiprazole had effects on PKA activity, GSK3β-dependent pathways, GABAA receptors, NMDA receptor and CREB1 in the brain. Since antipsychotics are used chronically in clinics, the present study investigated the long-term effects of chronic oral aripiprazole treatment on these cellular signalling pathways, in comparison with haloperidol (a D2R antagonist) and bifeprunox (a potent D2R partial agonist). We found that the Akt-GSK3β pathway was activated by aripiprazole and bifeprunox in the prefrontal cortex; NMDA NR2A levels were reduced by aripiprazole and haloperidol. In the nucleus accumbens, all three drugs increased Akt-GSK3β signalling; in addition, both aripiprazole and haloperidol, but not bifeprunox, increased the expression of Dvl-3, β-catenin and GABAA receptors, NMDA receptor subunits, as well as CREB1 phosphorylation
Detection of qnr in Clinical Isolates of Escherichia coli from Korea | Antimicrobial Agents and Chemotherapy
Quinolone resistance is usually caused by various chromosomal mutations that alter the target enzymes, such as DNA gyrase and topoisomerase IV, or activate efflux systems (2). Plasmid-mediated quinolone resistance has only recently been discovered (5). The plasmid gene responsible for quinolone resistance, termed qnr, is carried on class 1 integrons of the In4 family, downstream of the conserved region containing the orf513 recombinase gene (4, 10, 12), and encodes a 218-amino-acid protein that belongs to the pentapeptide-repeat family of proteins (10). The presence of qnr increases the resistance to nalidixic acid and fluoroquinolones by four- to eightfold (5).. The presence of the qnr gene in clinical isolates from Korea has not yet been reported. Therefore, in this study we screened for the presence of the qnr gene in clinical isolates of Escherichia coli from patients in Korea and analyzed the transferability and the genetic context of the qnr gene.. The presence of the qnr gene was screened ...
Influence of long-term oral application of quinolones on the ECG curve in dogs
The aim of the study was to analyse the influence of enrofloxacin and pradofloxacin administered orally for 14 days on the ECG in dogs. The ECG was performed before and after a 14 day period of quinolone administration. There was an increase in the QTc and the TpTe interval in the group treated with quinolones. QTc was prolonged by 24 ms (p=0.001). The TpTe interval was shortened, on average, by 6.55 ms (p=0.048). In the group treated with enrofloxacin, QTc was prolonged by 16.27 ms (p=0.006) and the TpTe interval was shortened by 9.64 ms (p=0.050), the TpTe/QT index was reduced by 0.034 (p=0.050) on average. In dogs treated with pradofloxacin, QTc was prolonged by 21.55 ms (p=0.012) on average. The results suggest that a prolonged administration of quinolones can increase the risk of arrhythmias. Furthermore, different generations of these drugs increase this risk to various degrees. The study proved that second generation quinolones, such as enrofloxacin, significantly change the phase of
Plasmid-mediated quinolone resistance in non-Typhi serotypes of Salmonella enterica. - PubMed - NCBI
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Previously, aripiprazole has been shown to be a partial agonist at the D2 dopamine receptor.The stabilizing effect of aripiprazole on the dopamine system was attributed to its targeting of presynaptic (auto-receptors) and post-synaptic D2 receptors. Therefore, it is effective to positive symptoms, negative symptoms as well as symptoms of cognitive impairments. In addition, aripiprazole is classified as a medication with significant 5HT2A-antagonism, and with still other additional secondary binding characteristics such as 5-HT2C, 5-HT7, epinephrine α1 and histamine H1 receptors. Its unique mechanism of action makes aripiprazole as a favorable clinical treatment choice over others, i.e. high efficacy, fewer extrapyramidal reactions (EPS), does not cause weight gain, does not cause the incensement of prolactin (PRL)[3, 12-13]. Consistently, our results showed that the overall response rate of aripiprazole treatment was 70.4 %, which was similar to that reported by Beijing Anding ...
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Lomefloxacin, a difluorinated quinolone derivative, is a bacterial gyrase inhibitor, effective against gram positive and gram negative bacteria. The acute toxicity of Lomefloxacin following systemic and topical ophthalmic application is low. Lomefloxacin interferes with bacterial DNA related processes like initiation, elongation, and termination phases of replication, transcription, DNA repairing, recombination, transposition, supercoiling and relaxation of DNA. The target molecule for quinolones is the A-subunit of bacterial enzyme gyrase (topoisomerase II). The forming of a stable complex between the quinolone and the whole gyrase teramer A2B2 leads to impaired enzyme functions, resulting in a rapid killing of sensitive bacteria.. Cross-resistance has only been reported with other quinolones, but not with any other group of antibiotics. No clinical studies are available about the efficacy in cases of infections with chlamydia.. ...
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Results Oral treatment with laquinimod (especially 0.5 mg/kg bw) not only improved motor impairment but also weight course and extended survival in R6/2 mice. R6/2 mice that were treated with 0.5 mg laquinimod showed longer life spans, as determined by Kaplan Meier analysis (p-value = 0.1). Upon analysis of motor performance, latency-to-fall values during rotarod testing in R6/2 mice were significantly different at the age of 12 weeks in the 0.5 and 25 mg/kg bw treated group (p*,0.05).. In the histological analysis, laquinimod treatment resulted in preservation of morphologically intact neurons in the motor cortex and striatum as revealed by neuronal marker NeuN and medium spiny neurons (MSNs) marker DARPP-32. Biochemical analysis also showed significant increase in brain derived neurotrophic factor (BDNF) level in the cortical (*p , 0.05) but not in striatal neurons. These effects seem to be mainly based on BDNF-pathways, influence on oxidative stress, and possibly reduction of ...
Open-label Study to Compare Hospitalization Rates of Schizophrenic Patients Treated With Oral Antipsychotics Versus IM Depot...
Patients who had no history of tolerability to oral aripiprazole received 10-15 mg/day (up to 30 mg/day) oral aripiprazole for 1 to 4 weeks to determine tolerability in the Tolerability Assessment Phase prior to receiving treatment with aripiprazole IM Depot. In the Open-label Aripiprazole IM Depot Phase, participants received aripiprazole intramuscular (IM) Depot 400 mg injection (dosage could be adjusted to 300 mg at the investigators discretion) monthly in the clinic for a total of 6 injections + concomitant oral aripiprazole 10-15 mg/day for the first 14 days. Participants at the investigators discretion were eligible to continue to receive aripiprazole IM depot (400 or 300 mg) injection monthly in the Open-label Aripiprazole IM Depot Extension phase. Oral aripiprazole was available as rescue medication if necessary ...
Squaring up to DNA: pentapeptide repeat proteins and DNA mimicry | SpringerLink
Antibiotics are considered one of the most crucial medical therapies available, and whether they are given for a simple urinary tract infection or for a serious disease, such as bacterial meningitis, the fact is that these medications have the capacity to eradicate a multitude of illnesses. Among the different antibiotic classes, the quinolone group (e.g. ciprofloxacin and levofloxacin) has risen as one of the most popular antibiotics, given that this class possesses remarkable versatility. They can easily wipe out pneumonia as well as obliterate harmful bacteria such as those that cause anthrax. Not surprisingly, following from their ample utility value, in 2010 the quinolones became the 5th most commonly prescribed antibiotic type within the U.S. However, this popularity and increase in antibiotic use contributed to our current issue with quinolone antibiotic resistance. In addition to this, the quinolones are known to be associated with an array of serious adverse effects, and patients taking ...
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PRIMARY OBJECTIVES:. I. To define the maximum tolerated dose (MTD) of R115777 (tipifarnib) in patients with relapsed, refractory, or high risk myeloid leukemias treated according to this regimen.. II. To assess the toxicity and preliminary assessment of efficacy of R115777 in patients with relapsed, refractory, or high risk myeloid leukemias.. OUTLINE: This is a dose-escalation, multicenter study.. Patients receive oral tipifarnib twice daily on days 1-7 and 15-21. Courses repeat every 28 days in the absence of unacceptable toxicity or disease progression. Patients achieving a complete response (CR) receive 2 additional courses beyond CR. Patients experiencing relapse after previously achieving CR may receive additional tipifarnib at the current dose level for newly registered patients.. Cohorts of 3-6 patients receive escalating doses of tipifarnib until the MTD is determined. The MTD is defined as the dose preceding that at which 2 of 3 or 2 of 6 patients experience dose-limiting ...
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An sRNA Screen for Reversal of Quinolone Resistance in Escherichia coli | G3: Genes | Genomes | Genetics
We carried out an sRNA screen to identify genes whose knockdown restores quinolone sensitivity in E. coli. Following an initial screen of ∼5000 sRNA-bearing clones, and secondary screening of over 500 clones, we found 30 genes whose disruption increases sensitivity of a gyrA S83L mutant by twofold or more. Our findings expand knowledge of the genetic interaction network of the essential gene gyrA, and provide potential targets for the development of antibiotic adjuvants to restore sensitivity in quinolone resistant pathogens.. Chemical-genetic sensitivity screens have largely used knockout approaches, whereby a library of knockout mutants is screened for sensitivity or resistance to an antibiotic at sub-lethal concentrations (e.g., Tamae et al. 2008; Breidenstein et al. 2008; Fajardo et al. 2008; Gomez and Neyfakh 2006; Liu et al. 2010). Typically, such screens are carried out on a wild-type, antibiotic susceptible background, so they are not well-suited to identifying genes whose knockdown ...
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Spectrophotometric Determination of Quinolones by Charge Transfer Complexation with Chloranilic Acid: Synthesis and...
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Hi Pat, I was told that it takes the counts longer to come up every time you have chomo and that after the first time the platelets are the most effected. I had Induction and then 30 days later a second round follow up round of 2 of the three drugsI had for induction. I too went into remission with the first round but so far I have not relapsed. It took my counts over 30 days to come back the second time. Then they put me on a Zarnestra trial for a year hoping to increase my chances of staying in remission. I am a little younger then your Mom-Im 63 & had no other medical problems. If you Mother is in remission again, you might check on the zarnestra trial going now in many places that is open to patients in a second remission but I do think they will want her counts up to a certain level. Barbras husband Ron is on that one. It is listed on the government list and is being run by Encologists instead of Hemos. I have had almost no side effect since they got the right dosage level for me. ...
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Palmatine Is a Plasmid-Mediated Quinolone Resistance (PMQR) Inhibitor That Restores the Activity of Ciprofloxacin Against QnrS and AAC(6ʹ)-Ib-cr-Producing Escherichia coli Peng Wang,1 Longfei Hu,1 Zhihui Hao2 1Agricultural Bio-Pharmaceutical Laboratory, Qingdao Agricultural University, Qingdao 266109, Peoples Republic of China; 2National Centre for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Beijing 100089, Peoples Republic of ChinaCorrespondence: Zhihui HaoNational Centre for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Beijing 100089, Peoples Republic of ChinaEmail [email protected]: The emergence of plasmid-mediated quinolone resistance (PMQR) is a global challenge in the treatment of clinical disease in both humans and animals and is exacerbated by the presence of different PMQR genes existing in the same bacterial strain. Here, we discovered that a natural isoquinoline alkaloid
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Quino-what?". We hear that a lot.. Before we explain what it is and why we are committed to helping victims, lets start with how it is pronounced.. Quinolone: kwĭnə-lōn. Fluoroquinolone: flu̇r-ō-ˈkwi-nə-ˌlōn\ History and difference between quinolones and fluoroquinolones.. The words quinolone and fluoroquinolone are often interchanged but there is a difference between the two. Both are terms for a class of antibiotics based on Nalidixic acid.. Nalidixic acid is the first of the synthetic quinolone antibiotics. It was discovered in 1962 by George Lesher and used clinically in 1967. Originally, in smaller doses Nalidixic acid inhibited growth and replication of bacteria; in higher doses it killed bacteria.. The addition of a fluorine atom is what differentiates quinolones from fluoroquinolones. Fluorine is an element; F2 on the Periodic Table. It is a toxic gas and is considered one of the most reactive elements. The addition of the fluorine atom and a piperazine ring make ...
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Chemical structure and pharmacokinetics of novel quinolone agents represented by avarofloxacin, delafloxacin, finafloxacin,...
Quinolones are potent synthetic antimicrobials first developed in the 1960s. Since then several agents have been synthetised by modification of basic bicyclic chemical structure. Quinolones and fluoroquinolones are classified based on their chemical structure, antibacterial spectrum and pharmacokinetic features. Each agent inhibits bacterial DNA synthesis by forming a ternary complex with a DNA molecule and gyrase and topoisomerase IV enzymes, thus blocking bacterial DNA supercoiling [1-3].. The first quinolone agents were nalidixic acid, cinoxacin and oxolinic acid, each had basic bicyclic quinolone ring. These agents achieved 20-40 mg/L peak serum concentrations (Cmax) after a treatment with doses of 500-1000 mg. These agents and their metabolites were excreted by kidney and they reached 500-1000 mg/L peak urine concentrations 2-4 h following adminstration. The narrow-spectrum activity of these quinolones limited their use in clinical practice [4, 5].. Substituents on certain part of quinolone ...
Arsenic in the structure of Crystal Structure of A Pentapeptide Repeat Protein (RFR23) From the Cyanobacterium Cyanothece 51142...
J Clin Psychiatry/Analysis of Suicidality in Pooled Data From 2 Double-Blind, Placebo-Controlled Aripiprazole Adjunctive...
Objective: To assess the impact of adjunctive aripiprazole versus adjunctive placebo treatment on suicidality in patients with major depressive disorder.. Method: Data were pooled from 2 identical aripiprazole augmentation studies. Patients with DSM-IV-TR-diagnosed major depressive disorder with an inadequate response to 8 weeks of prospective antidepressant treatment were randomly assigned to adjunctive placebo or adjunctive aripiprazole (2-20 mg/d) treatment for 6 weeks. Adverse events related to suicidality were identified in the adverse event database using the Medical Dictionary for Regulatory Activities-preferred term. Treatment-emergent suicidal ideation was defined using item 10 (suicidality) of the Montgomery-Åsberg Depression Rating Scale (MADRS) and item 18 (suicidality) of the Inventory of Depressive Symptomatology (IDS).. Results: In total, 737 patients were included in the safety database (aripiprazole n = 371; placebo n = 366). No suicides were reported. There were no ...
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids...
Positive Phase 3 Study Results for TRIKAFTA® (elexacaftor/tezacaftor/ivacaftor and ivacaftor) in People Ages 12 and Older With...
We look forward to submitting these data to the EMA in support of a potential indication expansion of the EU label following initial approval." About the 445-104 Study The data announced today are from a global Phase 3, randomized, double-blind, parallel-group study to evaluate the efficacy and safety of TRIKAFTA in people with CF ages 12 years and older who have one copy of the F508del mutation and one gating mutation (F/G), or one copy of the F508del mutation and one residual function mutation (F/RF). All participants had a 4-week run-in period of either ivacaftor or tezacaftor/ivacaftor. Following the run-in, patients were randomized to receive TRIKAFTA or to remain on their prior regimen of ivacaftor or tezacaftor/ivacaftor for 8 weeks. Baseline was measured at the end of the run-in period, prior to the start of the 8-week treatment period. A total of 132 participants received TRIKAFTA and 126 patients were in the control group that received either ivacaftor or tezacaftor/ivacaftor. The ...
Microbiological assay with Bacillus licheniformis for the easy detection of quinolones in milk - PubAg
This paper proposes a microbiological method in microtitre plates for the detection of residues of quinolones in milk. The method uses spores of Bacillus licheniformis in culture medium with a redox combination of indicators and gives a response time of 5.5 h. This method detects 92 μg L−1 of ciprofloxacin, 63 μg L−1 of danofloxacin, 109 μg L−1 of enrofloxacin, 101 μg L−1 of marbofloxacin and 109 μg L−1 of sarafloxacin in milk. Therefore, the assay is easy to develop and to use in laboratory, allowing analysis of large numbers of samples at low cost. Due to its good sensitivity to quinolones, this assay can be used as a complementary test of commercial microbiological methods and thereby improve food security ...
Indian Patents. 233059:'TRICYCLIC QUINOLINONE OR QUINOLINE-2(1H)-THIONE COMPOUNDS AS ANDROGEN RECEPTOR MODULATOR COMPOUNDS AND...
Intracellular receptors (IRs) form a class of structurally-related genetic regulators scientists have named "ligand dependent transcription factors." R.M. Evans, Science, 240:889 (1988). Steroid receptors are a recognized subset of the IRs, including the progesterone receptor (PR) androgen receptor (AR), estrogen receptor (ER), glucocorticoid receptor (GR) and mineralocorticoid receptor (MR). Regulation of a gene by such factors requires both the IR itself and a corresponding ligand, which has the ability to selectively bind to the IR in a way that affects gene transcription ...
Structure Elucidation and Preliminary Assessment of Hydrolase Activity of PqsE, the Pseudomonas Quinolone Signal (PQS)...
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A 52-week, haloperidol-controlled, long-term, maintenance trial (n=1294) was conducted in patients with acute relapse of chronic schizophrenia. In this trial involving the administration of aripiprazole 30 mg/day and haloperidol 10 mg/day, with a one-time option to decrease aripiprazole to 20 mg/day and haloperidol to 7 mg/day, aripiprazole was at least comparable to haloperidol in time-to-failure to maintain response in responders. Based on patients who responded at any time during the 52-week study (610/853, 72% in the aripiprazole group and 298/430, 69% in the haloperidol group), there was a 12% lower risk of subsequent failure with aripiprazole relative to haloperidol (relative risk: 0.881, 95% CI: 0.645 - 1.204). Aripiprazole was comparable to haloperidol in time-to-failure to maintain response in all randomized patients. Patients in the aripiprazole group had a 14% lower risk of failure compared with the haloperidol group (relative risk: 0.858, 95% CI: 0.721, 1.021). Aripiprazole was ...
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Discovery of a small molecule dihydroquinolinone inhibitor with potent antiproliferative and antitumor activity results in...
A family of dihydroquinolinones that inhibited the proliferation of a number of cancer cell lines and targeted the oncogenic activities of the late simian virus 40 factor (LSF) was discovered. The lead quinolinone inhibitors, 8-(2-propoxyphenyl)-7,8-dihydro-[1,3]dioxolo[4,5-g]quinolin-6(5H)-one, FQI1, and 8-(2-propoxyphenyl)-[1,3]dioxolo[4,5-g]quinolin-6(5H)-one, FQI2, were determined by a comprehensive SAR study. The lead compounds had low micromolar to nanomolar Gi50S and IC50S (concentrations that induced 50% inhibition) in cell growth and LSF-directed luciferase reporter assays, respectively. A distinct correlation between the GI50 and IC50 values indicated antiproliferative effects resulted from inhibition of LSF activity. FQI1 had no growth effects on immortalized human hepatocytes or primary mouse hepatocytes. Overall, FQI1 proved a good drug candidate for hepatocellular carcinoma (HCC). It possessed a low molecular weight and moderate solubility, which was improved by substitution of the ...
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Aripiprazole. Grady, Michelle A.; Gasperoni, Timothy L.; Kirkpatrick, Peter // Nature Reviews Drug Discovery;Jun2003, Vol. 2 Issue 6, p427 Focuses on the use of aripiprazole drugs in the treatment of schizophrenia. Properties of aripiprazole; Functionality of the drug; Impact of application of aripiprazole on schizophrenics; Definition of schizophrenia; Symptoms of the disease; Drugs previously used for the treatment of schizophrenia. ...
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A babys body and most internal organs are formed during the first 12 weeks of pregnancy. It is mainly during this time that some medicines are known to cause birth defects. Four well-designed studies all found that birth defects were no more common in babies born to pregnant women who took a quinolone antibiotic in early pregnancy than in babies of women not taking quinolones. One study that investigated whether use of a quinolone antibiotic in early pregnancy may increase the likelihood of specific types of heart defects found possible links with two types: conotruncal defects and tetralogy of Fallot. Because these study findings were based on small numbers of babies exposed in the womb they require confirmation with further research.. All of the four studies of women specifically using ciprofloxacin, and eight of nine studies of women using norfloxacin, found no increased occurrence of birth defects in their babies. Single studies specifically investigating levofloxacin, moxifloxacin, ...
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Endogenousmatrix interference using a similar m/z value is usually problematic. Many factors ought to be examined before an Tipifarnib method can be reliably applied to test analysis, especiallymultiple analytes with similar structures andmasses dont createa cross-talk phenomenon. Metabolites with a very close m/zvalue to that in the analyzed parent drug is usually problematicin SRM acquisition that will possibly be resolved just by highresolutionaccurate mass (HR) acquisition. Moreover, the selective nature of SRM acquisition can maskvaluable information including co-eluting matrix ions, degradationproducts or adducts with the analytes of interest.. It can have asignificant impact with assay quality and robustness when runninglarge number of various samples in some sort of routine manner. The mainadvantages ofHRover SRMacquisition in quantitative-qualitative(Quan-Qual) analyses have already been described. In add-on, the SRM-based approach is cumbersome not fast enoughto perform quantitation ...
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CO Norfloxacin - Uses, Side Effects, Interactions - Canada.com
CO Norfloxacin: Norfloxacin is an antibiotic that belongs to the class of medications called quinolones. It is used to treat infections caused by certain types of bacteria. It is most commonly used to treat urinary tract (bladder) infections. Norfloxacin works by killing some types of bacteria that can cause these infections.
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... , like other quinolones and fluoroquinolones, are bactericidal drugs, actively killing bacteria. Quinolones inhibit ... Quinolones can enter cells easily and therefore are often used to treat intracellular pathogens such as Legionella pneumophila ... Quinolones Psaty, BM. (Dec 2008). "Clinical trial design and selected drug safety issues for antibiotics used to treat ...
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 ...
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. ...
quinolones for community-acquired pneumonia: meta-analysis of randomized controlled trials". Clin. Microbiol. Infect. 19 (4): ... Drlica K, Zhao X (1 September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377- ... 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 ...
... 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). " ...
Quinolone Chidiac, C.; Mouton, Y. (1991). "Quinolones in the treatment of lower respiratory tract infections caused by ... Individuals with a history of hypersensitivity to quinolones should avoid this product. In humans, there is a risk of user ... Therefore, the concurrent oral administration of quinolones with foods, supplements or other preparations containing any of ... may substantially interfere with the absorption of quinolones from the intestinal tract resulting in decreased bioavailability ...
1992). "Cytotoxicity of quinolones toward eukaryotic cells. Identification of topoisomerase II as the primary cellular target ... Although the reaction product is often shown as a hydroxyquinoline (the enol form), it is believed that the quinolone (keto ... The synthesis of 4-hydroxyquinolines and 4-quinolones is of great importance to a variety of fields, but most notably to the ... there is some discrepancy on whether a substituted 4-hydroxyquinoline or a substituted 4-quinolone is the final product of the ...
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 ...
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However a recent investigation into the origin of quinolones have discovered that a description for quinolones happened in 1949 ... These include the quinolone class, of which nalidixic acid is often credited as the first to be discovered. Like other ... Emmerson, A. M.; Jones, A. M. (2003-05-01). "The quinolones: decades of development and use". Journal of Antimicrobial ... Bisacchi, Gregory S. (2015-06-25). "Origins of the Quinolone Class of Antibacterials: An Expanded "Discovery Story"". Journal ...
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 ...
Quinolones Murata K, Tokura Y (March 2007). "[Anti-microbial therapies for acne vulgaris: anti-inflammatory actions of anti- ... Nadifloxacin does not show cross-resistance with other new quinolones. Nadifloxacin inhibits the enzyme DNA gyrase that is ... Kuwahara K, Kitazawa T, Kitagaki H, Tsukamoto T, Kikuchi M (April 2005). "Nadifloxacin, an antiacne quinolone antimicrobial, ... risking the development of quinolone resistances. During the treatment some patients may develop some adverse effects ...
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: ...
Quinolones "Recalling the Omniflox (Temafloxacin) Tablets" (pdf). Food and Drug Administration. 1992-06-05. Retrieved 2014-10- ... Gentry LO (December 1991). "Review of quinolones in the treatment of infections of the skin and skin structure". J. Antimicrob ... Rubinstein, E. "History of quinolones and their side effects". Chemotherapy. 47 Suppl 3: 3-8; discussion 44-8. doi:10.1159/ ...
Synthetic quinolone antibiotics were discovered by George Lesher and coworkers as a byproduct of chloroquine manufacture in the ... In a technical sense, it is a naphthyridone, not a quinolone: its ring structure is a 1,8-naphthyridine nucleus that contains ... Amfonelic acid Oxolinic acid Emmerson AM, Jones AM (May 2003). "The quinolones: decades of development and use" (pdf). The ... Nalidixic acid (tradenames Nevigramon, Neggram, Wintomylon and WIN 18,320) is the first of the synthetic quinolone antibiotics ...
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- ... Drlica K, Zhao X (1 September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377- ... any member of the quinolone class of antimicrobial agents, or any of the product components." Though not stated as such within ...
Like all quinolones, it functions by inhibiting the DNA gyrase and topoisomerase IV. Topoisomerase IV is necessary to separate ... Drlica K, Zhao X (1 September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377- ... 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 ...
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Rifampicin can be used in combination with a quinolone or macrolide. It is uncertain whether rifampicin is an effective ... Effective antibiotics include most macrolides, tetracyclines, ketolides, and quinolones. Legionella multiply within the cell, ... Current treatments of choice are the respiratory tract quinolones (levofloxacin, moxifloxacin, gemifloxacin) or newer ... are prescribed for children above the age of 12 and quinolones (levofloxacin) above the age of 18. ...
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. ...
Overview of Quinolones (Example) - MindMeister
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. 220.127.116.11. gemifloxacin ...
Spectrophotometric Determination of Quinolones by Charge Transfer Complexation with Chloranilic Acid: Synthesis and...
Spectrophotometric Determination of Quinolones by Charge Transfer Complexation with Chloranilic Acid: Synthesis and ... A simple and sensitive spectrophotometric method has been described for the assay of quinolones in bulk drug and in ... The developed method is based on the formation of colored charge transfer complexes of quinolones with chloranilic acid in ... Spectrophotometric Determination of Quinolones by Charge Transfer Complexation with Chloranilic Acid: Synthesis and ...
An sRNA Screen for Reversal of Quinolone Resistance in Escherichia coli | G3: Genes | Genomes | Genetics
An sRNA Screen for Reversal of Quinolone Resistance in Escherichia coli. View ORCID ProfileKamya Bhatnagar, Aaron Hinz, Melissa ... An sRNA Screen for Reversal of Quinolone Resistance in Escherichia coli. View ORCID ProfileKamya Bhatnagar, Aaron Hinz, Melissa ... An sRNA Screen for Reversal of Quinolone Resistance in Escherichia coli. View ORCID ProfileKamya Bhatnagar, Aaron Hinz, Melissa ... 2004 Quinolones Antimicrobial Agents, 3rd Edition. Emerg. Infect. Dis. 10: 1177. doi:10.3201/eid1006.040025. ...
Indications of quinolone antibiotics restricted following EU-wide safety review | MIMS online
New restrictions and precautions for use have been implemented for quinolone antibiotics following very rare reports of ... Use of quinolones should be avoided in patients who have previously experienced serious adverse reactions with a quinolone. ... Quinolone warning over aortic aneurysm risk Quinolone antibiotics may be associated with an increased... ... Use of a corticosteroid with a quinolone should also be avoided as co-administration could exacerbate quinolone-induced ...
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T1 - Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations in quinolone-resistant ... Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations in quinolone-resistant ... Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations in quinolone-resistant ... title = "Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations in quinolone- ...
High incidence of plasmid-mediated quinolone resistance genes among ciprofloxacin-resistant clinical isolates of...
Plasmid-mediated quinolone resistance (PMQR) has received considerable attention recently. Data analysis in Jawaharlal ... Plasmid-mediated quinolone resistance genes, aac(6′)-Ib-cr, qnrS, qnrB, and qnrA, in urinary isolates of Escherichia coli and ... Plasmid-Mediated quinolone resistance in clinical isolates of escherichia coli from Shanghai, China.. Journal of Antimicrobial ... Plasmid-mediated quinolone resistance in typhoidal Salmonellae: a preliminary report from South India.. Indian Journal of ...
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Quinolones - A Powerful Friend if Used Sparingly. Posted on March 20, 2015. by Marisela ... The quinolones work by inhibiting the synthesis of bacterial DNA, a process which results in bacterial cell death. These ... The quinolone antibiotics should not be given to pregnant females or children, as they can cause cartilage damage. Additionally ... Quinolones are associated with a variety of significant complications, including: A) development of clostridium difficile ...
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Category:Quinolones - Wikimedia Commons
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 ... any chemical compound having 2-quinolone or 4-quinolone skeleton in its structure (en); chem. Verbindung(en) (de); Famile d ... quinolones (en); chinolony (pl); Kinoloner (nb); Quinolone, Quinolon, Quinolonen, Chinolonen (nl) ...
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 ...
Quinolone antibiotic - Wikipedia
Andriole, VT The Quinolones. Academic Press, 1989. *^ Andersson MI, MacGowan AP (2003). "Development of the quinolones". ... Although not formally a quinolone, nalidixic acid is considered the first quinolone drug. It was introduced in 1962 for ... A quinolone antibiotic is a member of a large group of broad-spectrum bactericides that share a bicyclic core structure related ... Quinolones are contraindicated if a patient has epilepsy, Ehlers-Danlos Syndrome, QT prolongation, pre-existing CNS lesions ...
Quinolone antibiotic - Wikipedia
Andriole, VT The Quinolones. Academic Press, 1989. *^ Andersson MI, MacGowan AP (2003). "Development of the quinolones". ... Quinolone antibiotic at Curlie (based on DMOZ). *Healthcare-associated Infections (HAIs)- Quinolones and the Clinical ... Norris, S; Mandell, GL (1988). "The quinolones: history and overview". The quinolones: history and overview. San Diego: ... Although not formally a quinolone, nalidixic acid is considered the first quinolone drug. It was introduced in 1962 for ...
Resultat #1550819 - GENOMIC CHARACTERIZATION AND COMPARISON OF QUINOLONE RESISTANT ESCHERICHIA COLI FROM POULTRY AND HUMANS IN...
Quinolone resistance despite low antimicrobial usage - mechanisms and possible preventive measures Anne Margrete Urdahl + 10 ... GENOMIC CHARACTERIZATION AND COMPARISON OF QUINOLONE RESISTANT ESCHERICHIA COLI FROM POULTRY AND HUMANS IN NORWAY ... GENOMIC CHARACTERIZATION AND COMPARISON OF QUINOLONE RESISTANT ESCHERICHIA COLI FROM POULTRY AND HUMANS IN NORWAY ...
Quinolones and the Clinical Laboratory | HAI | CDC
What are quinolones? Quinolones are antimicrobial agents effective in the treatment of selected community-acquired and ... How does resistance to quinolones develop? Quinolones inhibit two enzymes that are required for bacterial DNA synthesis, i.e., ... What organisms can be resistant to quinolones? Resistance to quinolones has been reported in a variety of important bacterial ... Resistance to quinolones limits drug selection for treatment of many infections.. *Organisms resistant to quinolones often are ...
4-Quinolone - Wikipedia
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 4-quinolone antibiotics represent a large class of important drugs. The chemical synthesis of quinolones often involves ... 4-Quinolone is an organic compound derived from quinoline. ... 4-Quinolone is of little intrinsic value but its derivatives, ...
Interactions between Insulin Regular Human Injection and antidiabetic-agents-selected-quinolones
... provides information about interactions between Insulin Regular Human Injection and antidiabetic-agents-selected-quinolones. ... Antidiabetic Agents/Selected Quinolones. This information is generalized and not intended as specific medical advice. Consult ... Using some quinolone antibiotics with your diabetes medicine may make your blood sugar too low. ...
Structural development, haematological immunological and pharmacological effects of quinolones. - PubMed - NCBI
The constant need for new anti microbials has produced a variety of newer quinolones termed as I, II, III, and IV generation. ... The interest of the medical community in quinolones has not decreased despite more than ten years of continuous and growing use ... Structural development, haematological immunological and pharmacological effects of quinolones.. Chide OE1, Orisakwe OE. ... These attributes, coupled with their expanded spectrum and the immune enhancing phenomena of quinolones with a cyclopropyl ...
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... provides information about interactions between Glyburide-Metformin Oral and selected-antidiabetic-agents-selected-quinolones. ... Using some quinolone antibiotics with your diabetes medicine may make your blood sugar too low. ... Selected Antidiabetic Agents/Selected Quinolones Interactions. This information is generalized and not intended as specific ...
Topoisomerase IV is a target of quinolones in Escherichia coli | PNAS
Topoisomerase IV is a target of quinolones in Escherichia coli. A B Khodursky, E L Zechiedrich, and N R Cozzarelli ... We suggest that this and a slightly higher intrinsic resistance of topo IV make it secondary to gyrase as a quinolone target. ... Our results imply that the quinolone binding pockets of gyrase and topo IV are similar and that substantial levels of drug ... Mutant forms of topo IV provided an additional 10-fold resistance to quinolones and prevented drug-induced catenane ...
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Antibiotic, Quinolone. Class Summary. The quinolone class antibiotics are no longer considered effective against GCU due to ... 45] Quinolone-resistant GCU is also more prevalent in men who have sex with men. Because of increasing resistance, quinolones ( ... Quinolone resistance has increase worldwide, now approximately 21%,  and is common in Asia, the Pacific, Europe, and the ... 54, 55, 56] although there is concern for emerging quinolone resistance [5, 18, 15, 16] ). Other choices could include 7 days ...
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Quinolones: A Comprehensive Review - American Family Physician
Quinolones have few adverse effects, most notably nausea, headache, dizziness, and confusion. Less common but more serious ... Most quinolones have excellent oral bioavailability, with serum drug concentrations equivalent to intravenous administration. ... Comparison of Quinolone Generations. Quinolone generations. Microbiologic activity. Administration and characteristics. ... Comparison of Quinolone Generations. Quinolone generations. Microbiologic activity. Administration and characteristics. ...
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Endochin-like quinolones are highly efficacious against acute and latent experimental toxoplasmosis | PNAS
Recent 4-(1H)-quinolone derivatives, endochin-like quinolones (ELQ), exhibit an in vitro IC50 against Plasmodium falciparum as ... Endochin-like quinolones against Toxoplasma. J. Stone Doggett, Aaron Nilsen, Isaac Forquer, Keith W. Wegmann, Lorraine Jones- ... Endochin-like quinolones against Toxoplasma. J. Stone Doggett, Aaron Nilsen, Isaac Forquer, Keith W. Wegmann, Lorraine Jones- ... quinolone-3-diarylethers was made to improve these properties. Of the 4(1H)-quinolone-3-diarylethers synthesized in our ...
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Buy the Hardcover Book The Quinolones by Vincent T. Andriole at Indigo.ca, Canadas largest bookstore. + Get Free Shipping on ... Use of the Quinolones in Sexually Transmitted Diseases. Treatment of Respiratory Infections with Quinolones. Use of Quinolones ... Use of the Quinolones in Treatment of Bacterial Meningitis. Use of the Quinolones in Immunocompromised Patients. Use of the ... The Quinolones: History and Overview. Chemistry and Mechanism of Action of the Quinolone Antibacterials. Comparative In-Vitro ...
Antibiotics | Free Full-Text | Our Evolving Understanding of the Mechanism of Quinolones
In this review, we present hallmark investigations describing the mode of action of quinolones, one of the antibacterial ... the necessity to look beyond primary drug-target interactions towards thoroughly understanding the mechanism of quinolones at ... Keywords: antibiotics; quinolones; topoisomerases; DNA replication; DNA supercoiling antibiotics; quinolones; topoisomerases; ... Gutierrez, A.; Stokes, J.M.; Matic, I. Our Evolving Understanding of the Mechanism of Quinolones. Antibiotics 2018, 7, 32. ...
Quinolone-Containing Therapies in the Eradication of Helicobacter pylori
... Seng-Kee Chuah,1 Wei-Chen Tai,1 Chen-Hsiang Lee,2 ... W. L. Chang, C. Y. Kao, C. T. Wu et al., "Gemifloxacin can partially overcome quinolone resistance of H. pylori with gyrA ... A. Robicsek, G. A. Jacoby, and D. C. Hooper, "The worldwide emergence of plasmid-mediated quinolone resistance," The Lancet ... M. Berning, S. Krasz, and S. Miehlke, "Review: should quinolones come first in Helicobacter pylori therapy?" Therapeutic ...
The Quinolones | Annals of Internal Medicine | American College of Physicians
The New Fluorinated Quinolones for Infection Prevention in Acute Leukemia Annals of Internal Medicine; 106 (1): 144-146 ... Oral Quinolone Treatment for Osteomyelitis Annals of Internal Medicine; 115 (10): 832 ... Quinolone-Based Antibacterial Chemoprophylaxis in Neutropenic Patients: Effect of Augmented Gram-Positive Activity on ... Development and bioanalytical method validation of an LC-MS/MS assay for simultaneous quantitation of 2-alkyl-4(1H)-quinolones ...
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Reduction of the fitness burden of quinolone resistance in Pseudomonas aeruginosa. - PubMed - NCBI
Reduction of the fitness burden of quinolone resistance in Pseudomonas aeruginosa.. Kugelberg E1, Löfmark S, Wretlind B, ... Quinolone resistance in the opportunistic pathogen Pseudomonas aeruginosa is commonly caused by mutations that alter the target ... We have analysed the effect of quinolone resistance caused by DNA gyrase/topoisomerase IV mutations on bacterial fitness. ... Our results show that no cost and compensatory mutations are common in quinolone-resistant P. aeruginosa. ...
Quinolones, including Fluoroquinolones - Pharmacology - Merck Veterinary Manual
Learn about the veterinary topic of Quinolones, including Fluoroquinolones. Find specific details on this topic and related ... Examples of the quinolone carboxylic acids and species in which they are approved are presented in Quinolones and Species ... Most quinolones also cross the placental barrier. The apparent volume of distribution of most quinolones is large. The degree ... Known generically as quinolones or 4-quinolones, these drugs are derived from several closely related ring structures that have ...
The broad-spectrum quinolones are here†
These agents have extended spectra of antibacterial activity compared with the earlier quinolones such as ciprofloxacin and ... IN BRIEFThere are now a selection of broad-spectrum quinolones available which are likely to be used as first-line agents ... the quinolones can cause some serious adverse effects and the adverse effect profiles of these newer quinolones are not ... IN BRIEFThere are now a selection of broad-spectrum quinolones available which are likely to be used as first-line agents ...
Correction: A robust iron catalyst for the selective hydrogenation of substituted (iso)quinolones - Chemical Science (RSC...
... quinolones by Basudev Sahoo et al., Chem. Sci., 2018, DOI: 10.1039/c8sc02744g. ... Correction for A robust iron catalyst for the selective hydrogenation of substituted (iso)quinolones by Basudev Sahoo et al. ... Correction: A robust iron catalyst for the selective hydrogenation of substituted (iso)quinolones B. Sahoo, C. Kreyenschulte, G ... Correction: A robust iron catalyst for the selective hydrogenation of substituted (iso)quinolones ...
... 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; ...
Gram-Positive Infections and Quinolones in Neutropenia | Annals of Internal Medicine | American College of Physicians
Regulation of Pseudomonas Quinolone Signal Synthesis in Pseudomonas aeruginosa | Journal of Bacteriology
A third intercellular signal, the Pseudomonas quinolone signal (PQS; 2-heptyl-3-hydroxy-4-quinolone), also regulates numerous ... Regulation of Pseudomonas Quinolone Signal Synthesis in Pseudomonas aeruginosa. Dana S. Wade, M. Worth Calfee, Edson R. Rocha, ... Regulation of Pseudomonas Quinolone Signal Synthesis in Pseudomonas aeruginosa. Dana S. Wade, M. Worth Calfee, Edson R. Rocha, ... aeruginosa intercellular signal is a quinolone compound that was identified as 2-heptyl-3-hydroxy-4-quinolone (the Pseudomonas ...
Conferring quinolone resistanceIsolatesAntibioticsGyraseEscherichiaVitro activityPMQRResistance determiPlasmidEnrofloxacinSynthesisComplexesAdverse effectsGyrAOccurArrhythmiasPharmaceuticalTargetRiskGroupPreviouslyFluoroquinolonesNalidixicSalmonellaGenesCarboxylic acidFluoroquinoloneResistantVitroStrainsMutation in the quinoloneNewerMechanismField of quinolonePatients taking quiEffects of quinolonesColiEffect of quinoloneDetermination of quinolonesTopoisomerasesBactericidalSystemicAmino acid mutationsOfloxacinNovel quinoloneVarious quinolonesPlasmidSyntheticInteractions
Conferring quinolone resistance1
- The aim of the study was to investigate the prevalence of plasmid-mediated quinolone resistance (PMQR) genes in an unselected collection of bloodstream isolates recovered over an 18-month period in a laboratory affiliated to a university hospital in Athens, Greece, and to assess their impact on the in vitro activity of ciprofloxacin and levofloxacin. (microbiologyresearch.org)
- New restrictions and precautions for use have been implemented for quinolone antibiotics following very rare reports of disabling, long-lasting or potentially irreversible adverse reactions affecting the musculoskeletal and nervous systems. (mims.co.uk)
- The decision by the Medicines and Healthcare products Regulatory Agency (MHRA) to restrict the indications for quinolone antibiotics was based on recommendations from the the European Medicines Agency's (EMA's) Pharmacovigilance Risk Assessment Committee after it conducted a review of serious adverse effects reported with the use of quinolones given orally, parenterally or by inhalation. (mims.co.uk)
- Quinolone antibiotics are authorised for serious, life-threatening bacterial infections. (mims.co.uk)
- Quinolone antibiotics may be associated with an increased. (mims.co.uk)
- Cross-resistance has only been reported with other quinolones, but not with any other group of antibiotics. (com.bd)
- Lomefloxacin, a difluorinated quinolone derivative, is a bacterial gyrase inhibitor, effective against gram positive and gram negative bacteria. (com.bd)
- The target molecule for quinolones is the A-subunit of bacterial enzyme gyrase (topoisomerase II). (com.bd)
- The forming of a stable complex between the quinolone and the whole gyrase teramer A2B2 leads to impaired enzyme functions, resulting in a rapid killing of sensitive bacteria. (com.bd)
- 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)
- The presence of a single PMQR determinant without any target modification was not associated with quinolone resistance with one exception, S tenotrophomonas maltophilia carrying qnrS1 , which was resistant to norfloxacin and ciprofloxacin, but in this isolate, additional mechanisms of quinolone resistance cannot be excluded. (microbiologyresearch.org)
- The worldwide emergence of plasmid-mediated quinolone resistance. (microbiologyresearch.org)
- Plasmid-mediated quinolone resistance. (microbiologyresearch.org)
- Martínez-Martínez L , Pascual A , García I , Tran J , Jacoby GA . Interaction of plasmid and host quinolone resistance. (microbiologyresearch.org)
- Martínez-Martínez L , Pascual A , Jacoby GA . Quinolone resistance from a transferable plasmid. (microbiologyresearch.org)
- These attributes, coupled with their expanded spectrum and the immune enhancing phenomena of quinolones with a cyclopropyl moiety at position 1 of the quinolone ring suggest that the newer fluoroquinolones are so far the most ideal agents for the empirical treatment of many common infections. (nih.gov)
- Quinolones, and especially fluoroquinolones, are one of the largest classes of antibacterial agents used worldwide. (bl.uk)
- However, in recent years, this type of quinolone resistance was more frequently observed in animals to which more quinolones and fluoroquinolones were administered (broiler chickens and veal calves). (wur.nl)
- The association between fluoroquinolones and arthropathy was primarily described in immature animals, and only rarely in humans, yet it has led to the restricted use of quinolones during pregnancy. (springer.com)
- Resistance to quinolones and fluoroquinolones has been increasingly reported among human and veterinary isolates during the last three decades related to their wide clinical use. (eurekaselect.com)
- METHODS: Databases of national reference laboratories containing MIC values for Salmonella and E. coli isolated between 1994 and 2009 in animals, humans, food and the environment from 13 European countries were screened for isolates exhibiting a defined quinolone resistance phenotype, i.e. reduced susceptibility to fluoroquinolones and nalidixic acid. (dtu.dk)
- The first generation of the quinolones begins with the introduction of nalidixic acid in 1962 for treatment of urinary tract infections in humans. (princeton.edu)
- Early quinolones, such as nalidixic acid, had poor systemic distribution and limited activity and were used primarily for Gram-negative urinary tract infections. (cdc.gov)
- Nalidixic acid and other early quinolones had limited use due to poor pharmacokinetics, relatively narrow antimicrobial spectrum of activity, and frequent adverse effects. (nih.gov)
- The first quinolone, nalidixic acid (NegGram), was introduced in 1962. (aafp.org)
- Nalidixic acid, considered a first-generation drug, is the earliest of the quinolones. (merckvetmanual.com)
- Nalidixic acid was the less active quinolone. (eurekamag.com)
- Prevalence of quinolone resistance mechanisms and associations to minimum inhibitory concentrations (MICs) of nalidixic acid (NAL) and ciprofloxacin (CIP) were investigated in 124 Escherichia coli isolated from humans (n = 85) and swine (n = 39) in Denmark. (dtu.dk)
- Provides information on a study that monitored resistance to the drug quinolones in Salmonella enterica serotype enteritidis from human infections. (ebscohost.com)
- The acquisition of quinolone-resistance in E. coli and Salmonella has also been investigated. (bl.uk)
- In his research, Veldman describes the first Salmonella and E. coli bacteria with transferable quinolone resistance in farm animals and humans in the Netherlands. (wur.nl)
- Resistance to quinolones occurs through chromosomal mutations in the genes encoding these enzymes and by porin and efflux mutations. (cdc.gov)
- The opportunistic human pathogen secretes 2-heptyl-3-hydroxy-4-quinolone (PQS), a quorum sensing (QS) signal that regulates the expression of numerous virulence genes. (bioportfolio.com)
- The emergence of plasmid-mediated quinolone resistance (PMQR) is a global challenge in the treatment of clinical disease in both humans and animals and is exacerbated by the presence of different PMQR genes existing in the same bacterial strain. (dovepress.com)
- This study proposed to investigate the frequency of quinolone-resistance plasmid genes and the O-antigen serogroup among UPEC isolated from KTPs and non-KTP with UTI. (hindawi.com)
- The extent of quinolone-resistant genes in gram-negative bacteria like UPEC is a big concern for KTPs [ 1 ]. (hindawi.com)
- This study aimed to determine the genes coding for ESBLs, plasmid mediated quinolone resistance and virulence markers in commensal E. coli isolated from healthy school children. (diva-portal.org)
- To identify mutations in the gyrA and parC genes of the gonococcal mutants, the quinolone resistance determining regions of the gyrA and parC genes were polymerase chain reaction (PCR) amplified and the PCR products were directly sequenced. (bmj.com)
- Five plasmid-mediated quinolone resistance (PMQR) genes, qnrA, qnrB, qnrS, qepA, and aac(6')-Ib-cr, and the minimal inhibitory concentration (MIC) values for ciprofloxacin were tested for all the strains. (medworm.com)
- OBJECTIVES: We investigated the distribution of plasmid-mediated quinolone resistance (PMQR) genes from swine feedlots and their surrounding environment. (thefreedictionary.com)
- Twenty-one ciprofloxacin-resistant strains were analysed for mutations in quinolone resistance-determining regions (QRDR), acquired quinolone resistance (AQR) genes and the role of efflux pumps in resistance. (microbiologyresearch.org)
- Quinolone carboxylic acid derivatives are synthetic antimicrobial agents. (merckvetmanual.com)
- 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)
- The 7-bromoquinolone analogue, 7-bromo-6-(N-benzylpiperazin-1-yl)-4-oxo-3- quinolone carboxylic acid 91 showed the high potency as antibacterial inhibitor in addition to a significant effect on vitiligo phototherapy treatment. (bl.uk)
- 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)
- These were characterised using the genotypic methods of Plasmid Profile Analysis and Pulsed Field Gel Electrophoresis and levels of resistance were determined for quinolone and fluoroquinolone antimicrobials by the agar dilution method. (gla.ac.uk)
- The prevalence of mutations in the quinolone resistance determining region (QRDR) area in S epidermidis isolated from the ocular surface and its association with fluoroquinolone resistance has not been fully elucidated. (pubmedcentralcanada.ca)
- Organisms resistant to quinolones often are resistant to other classes of antimicrobials. (cdc.gov)
- Many resistant organisms have multiple enzyme target site, porin, and efflux mutations, producing high-level resistance to quinolones. (cdc.gov)
- Can an isolate be resistant to one quinolone and susceptible to another? (cdc.gov)
- [ 45 ] Quinolone-resistant GCU is also more prevalent in men who have sex with men. (medscape.com)
- Our results show that 'no cost' and compensatory mutations are common in quinolone-resistant P. aeruginosa. (nih.gov)
- The CRISPR/Cas9 system was used to generate gyrA mutations in quinolone-susceptible E. coli ATCC 25922, and quinolone-resistant clinical E. coli. (bioportfolio.com)
- The study's authors said a few individuals traveling outside the region may have been exposed to quinolones and on return transmitted resistant organisms to their neighbors. (thefreedictionary.com)
- We show that the endochin-like quinolone (ELQ) class of compounds contains extremely potent inhibitors of T. gondii growth in vitro and is effective against acute and latent toxoplasmosis in mice. (pnas.org)
- Following on from the finding that the complex of quinolone and gyrase on DNA results in truncated mRNAs in vitro, the results presented in this thesis show that in vivo, the addition of quinolone drugs results in the production of truncated mRNAs which are presumably translated into truncated proteins. (bl.uk)
- Evaluates the in vitro activity of seven quinolones against non-glucose fermenting Gram-negative bacilli isolated from clinical specimens of cancer patients. (ebscohost.com)
- The in vitro activity of eight antimicrobial agents, including four quinolones, against 108 strains of enteropathogens was determined. (eurekamag.com)
- Recent publications report in vitro activity of quinolone 3-esters against the bc1 protein complex of Plasmodium falciparum and the parasite. (unl.pt)
- All strains were susceptible to the quinolones. (eurekamag.com)
- The gyrA mutations causing changes at amino acids 83 and 87 reversed the features of quinolone resistance in ATCC and clinical strains, verifying the causal role of gyrA mutation in the quinolone resistance of E. coli. (bioportfolio.com)
Mutation in the quinolone1
- While studies indicated the relationship between gyrA mutations and bacterial resistance to quinolones, CRISPR/Cas9 was used in this study to investigate causal role of gyrA mutation in the quinolone resistance. (bioportfolio.com)
- The constant need for new anti microbials has produced a variety of newer quinolones termed as I, II, III, and IV generation. (nih.gov)
- Although generally well tolerated, the quinolones can cause some serious adverse effects and the adverse effect profiles of these newer quinolones are not identical. (ovid.com)
- All of the newer quinolones are effective against a wide range of organisms and will need to be used with care in an attempt to minimise the emergence of resistance to these agents. (ovid.com)
- Activity of the newer quinolones against Chlamydia trachomatis. (bmj.com)
- Most cephalosporins, except for Rocephin, need to be administered every eight hours, while the newer quinolones are administered once daily. (managedcaremag.com)
- It has also been shown that the newer more potent quinolone drugs such as ciprofloxacin and ofloxacin have an additional effect on the bacterial cells in that the chromosome is broken down into fragments of DNA, some of which are estimated to be as small as 4kb in length. (bl.uk)
- Gutierrez A, Stokes JM, Matic I. Our Evolving Understanding of the Mechanism of Quinolones. (mdpi.com)
- Both enzymes use a double-strand DNA passage mechanism, and it is likely that quinolone biochemistry is similar for both. (asm.org)
- As expected, target mutation in QRDRs was the most prevalent mechanism of quinolone resistance. (dtu.dk)
Field of quinolone1
Patients taking qui1
- Aortic ruptures or aneurysms in patients taking quinolones was increased by 66% over those taking amoxicillin within that most at-risk 60-day time period mentioned above. (regenexx.com)
Effects of quinolones3
- Structural development, haematological immunological and pharmacological effects of quinolones. (nih.gov)
- The thrust of this review is on the structural development, pharmacological, haematological and immunological effects of quinolones. (nih.gov)
- Effects of Quinolones on the Immune System, p 467-473. (asmscience.org)
Effect of quinolone1
Determination of quinolones1
- Multiclass method for the determination of quinolones and β-lactams, in raw cow milk using dispersive liquid-liquid microextraction and ultra high performance liquid chromatography-tandem mass spectrometry. (sigmaaldrich.com)
- Resistance studies revealed partial cross-resistance with fluoro-quinolones (FQs) suggesting that IPYs bind to the same region of bacterial topoisomerases as FQs and interact with at least some of the keys residues involved in FQ binding. (bioportfolio.com)
- In a sense, quinolones trap the bacterial type II topoisomerases on DNA ( 17 , 23 , 73 , 75 ) (Fig. 1 , step b 2 ). (asm.org)
- Simultaneously, systemic quinolone therapy rose from 28 percent in 1998 to over 56 percent in 2002. (managedcaremag.com)
- The MHRA advises prescribers that systemic quinolones can very rarely cause long-lasting (up to months or years), disabling, and potentially irreversible adverse reactions, sometimes affecting multiple systems, organ classes and senses. (mims.co.uk)
Amino acid mutations1
- Because of increasing resistance, quinolones (eg, ciprofloxacin 500 mg PO single dose, levofloxacin 250 mg PO single dose, or ofloxacin 400 mg PO single dose) are not currently recommended by the Centers for Disease Control and Prevention (CDC) for routine or alternative regimens. (medscape.com)
- These agents have extended spectra of antibacterial activity compared with the earlier quinolones such as ciprofloxacin and ofloxacin. (ovid.com)
- Reporting susceptibilities to various quinolones provides the information necessary to choose an appropriate therapy that will minimize the selection of mutations leading to resistance. (cdc.gov)
- Liquid formulations of various quinolones for PO or parenteral administration usually contain freely soluble salts in stable aqueous solutions. (merckvetmanual.com)
- This is one of the conclusions of a thesis entitled 'Plasmid mediated quinolone resistance in Enterobacteriaceae' by Kees Veldman, a researcher at CVI. (wur.nl)
- Vincent Cattoir and Patrice Nordmann, " Plasmid-Mediated Quinolone Resistance in Gram-Negative Bacterial Species: An Update", Current Medicinal Chemistry (2009) 16: 1028. (eurekaselect.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)