Computer Security: Protective measures against unauthorized access to or interference with computer operating systems, telecommunications, or data structures, especially the modification, deletion, destruction, or release of data in computers. It includes methods of forestalling interference by computer viruses or so-called computer hackers aiming to compromise stored data.Confidentiality: The privacy of information and its protection against unauthorized disclosure.Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.Privacy: The state of being free from intrusion or disturbance in one's private life or affairs. (Random House Unabridged Dictionary, 2d ed, 1993)Portal Vein: A short thick vein formed by union of the superior mesenteric vein and the splenic vein.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.Software: Sequential operating programs and data which instruct the functioning of a digital computer.Heterocyclic Compounds: Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)Internet: A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.Hypertension, Portal: Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN.Terminology as Topic: The terms, expressions, designations, or symbols used in a particular science, discipline, or specialized subject area.Safety: Freedom from exposure to danger and protection from the occurrence or risk of injury or loss. It suggests optimal precautions in the workplace, on the street, in the home, etc., and includes personal safety as well as the safety of property.Accidents, Occupational: Unforeseen occurrences, especially injuries in the course of work-related activities.Databases, Chemical: Databases devoted to knowledge about specific chemicals.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.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.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Manufactured Materials: Substances and materials manufactured for use in various technologies and industries and for domestic use.Equilenin: An estrogenic steroid produced by HORSES. It has a total of five double bonds in the A- and B-ring. High concentration of equilenin is found in the URINE of pregnant mares.Marketing: Activity involved in transfer of goods from producer to consumer or in the exchange of services.Chemical Industry: The aggregate enterprise of manufacturing and technically producing chemicals. (From Random House Unabridged Dictionary, 2d ed)Health Care Sector: Economic sector concerned with the provision, distribution, and consumption of health care services and related products.Drug Industry: That segment of commercial enterprise devoted to the design, development, and manufacture of chemical products for use in the diagnosis and treatment of disease, disability, or other dysfunction, or to improve function.Economic Competition: The effort of two or more parties to secure the business of a third party by offering, usually under fair or equitable rules of business practice, the most favorable terms.Marketing of Health Services: Application of marketing principles and techniques to maximize the use of health care resources.Commerce: The interchange of goods or commodities, especially on a large scale, between different countries or between populations within the same country. It includes trade (the buying, selling, or exchanging of commodities, whether wholesale or retail) and business (the purchase and sale of goods to make a profit). (From Random House Unabridged Dictionary, 2d ed, p411, p2005 & p283)Tobacco Industry: The aggregate business enterprise of agriculture, manufacture, and distribution related to tobacco and tobacco-derived products.Toxoplasma: A genus of protozoa parasitic to birds and mammals. T. gondii is one of the most common infectious pathogenic animal parasites of man.Qi: The vital life force in the body, supposedly able to be regulated by acupuncture. It corresponds roughly to the Greek pneuma, the Latin spiritus, and the ancient Indian prana. The concept of life-breath or vital energy was formulated as an indication of the awareness of man, originally directed externally toward nature or society but later turned inward to the self or life within. (From Comparison between Concepts of Life-Breath in East and West, 15th International Symposium on the Comparative History of Medicine - East and West, August 26-September 3, 1990, Shizuoka, Japan, pp. ix-x)Antimycin A: An antibiotic substance produced by Streptomyces species. It inhibits mitochondrial respiration and may deplete cellular levels of ATP. Antimycin A1 has been used as a fungicide, insecticide, and miticide. (From Merck Index, 12th ed)Toxoplasmosis: The acquired form of infection by Toxoplasma gondii in animals and man.Toxoplasmosis, Animal: Acquired infection of non-human animals by organisms of the genus TOXOPLASMA.Blogging: Using an INTERNET based personal journal which may consist of reflections, comments, and often hyperlinks.Babesiosis: A group of tick-borne diseases of mammals including ZOONOSES in humans. They are caused by protozoa of the genus BABESIA, which parasitize erythrocytes, producing hemolysis. In the U.S., the organism's natural host is mice and transmission is by the deer tick IXODES SCAPULARIS.Toxoplasmosis, Congenital: Prenatal protozoal infection with TOXOPLASMA gondii which is associated with injury to the developing fetal nervous system. The severity of this condition is related to the stage of pregnancy during which the infection occurs; first trimester infections are associated with a greater degree of neurologic dysfunction. Clinical features include HYDROCEPHALUS; MICROCEPHALY; deafness; cerebral calcifications; SEIZURES; and psychomotor retardation. Signs of a systemic infection may also be present at birth, including fever, rash, and hepatosplenomegaly. (From Adams et al., Principles of Neurology, 6th ed, p735)Toxoplasmosis, Ocular: Infection caused by the protozoan parasite TOXOPLASMA in which there is extensive connective tissue proliferation, the retina surrounding the lesions remains normal, and the ocular media remain clear. Chorioretinitis may be associated with all forms of toxoplasmosis, but is usually a late sequel of congenital toxoplasmosis. The severe ocular lesions in infants may lead to blindness.Nedocromil: A pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with ASTHMA, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets.Mast Cells: Granulated cells that are found in almost all tissues, most abundantly in the skin and the gastrointestinal tract. Like the BASOPHILS, mast cells contain large amounts of HISTAMINE and HEPARIN. Unlike basophils, mast cells normally remain in the tissues and do not circulate in the blood. Mast cells, derived from the bone marrow stem cells, are regulated by the STEM CELL FACTOR.Eosinophils: Granular leukocytes with a nucleus that usually has two lobes connected by a slender thread of chromatin, and cytoplasm containing coarse, round granules that are uniform in size and stainable by eosin.Cromolyn Sodium: A chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.Asthma: A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).Neutrophils: Granular leukocytes having a nucleus with three to five lobes connected by slender threads of chromatin, and cytoplasm containing fine inconspicuous granules and stainable by neutral dyes.Anti-Asthmatic Agents: Drugs that are used to treat asthma.Macrophages: The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)Asthma, Exercise-Induced: Asthma attacks following a period of exercise. Usually the induced attack is short-lived and regresses spontaneously. The magnitude of postexertional airway obstruction is strongly influenced by the environment in which exercise is performed (i.e. inhalation of cold air during physical exertion markedly augments the severity of the airway obstruction; conversely, warm humid air blunts or abolishes it).
(1/269) In vitro activities of cephalosporins and quinolones against Escherichia coli strains isolated from diarrheic dairy calves.

The in vitro activities of several cephalosporins and quinolones against 195 strains of Escherichia coli isolated from diary calves affected by neonatal diarrhea were determined. One hundred thirty-seven of these strains produced one or more potential virulence factors (F5, F41, F17, cytotoxic necrotizing factor, verotoxin, and the eae gene), but the remaining 58 strains did not produce any of these factors. From 11 to 18% of the E. coli strains were resistant to cephalothin, nalidixic acid, enoxacin, and enrofloxacin. However, cefuroxime, cefotaxime, and cefquinome were highly effective against the E. coli isolates tested. Some significant differences (P < 0.05) in resistance to quinolones between the strains producing potential virulence factors and nonfimbriated, nontoxigenic, eae-negative strains were found. Thus, eae-positive, necrotoxigenic, and verotoxigenic (except for nalidixic acid) E. coli strains were significantly more sensitive to nalidixic acid, enoxacin, and enrofloxacin than nonfimbriated, nontoxigenic, eae-negative strains. Moreover, eae-positive strains were significantly more sensitive to enoxacin and enrofloxacin than F5-positive strains. Thus, the result of this study suggest that the bovine E. coli strains that produce some potential virulence factors are more sensitive to quinolones than those that do not express these factors.  (+info)

(2/269) Cloning, expression, and enzymatic characterization of Pseudomonas aeruginosa topoisomerase IV.

The topoisomerase IV subunit A gene, parC homolog, has been cloned and sequenced from Pseudomonas aeruginosa PAO1, with cDNA encoding the N-terminal region of Escherichia coli parC used as a probe. The homolog and its upstream gene were presumed to be parC and parE through sequence homology with the parC and parE genes of other organisms. The deduced amino acid sequence of ParC and ParE showed 33 and 32% identity with that of the P. aeruginosa DNA gyrase subunits, GyrA and GyrB, respectively, and 69 and 75% identity with that of E. coli ParC and ParE, respectively. The putative ParC and ParE proteins were overexpressed and separately purified by use of a fusion system with a maltose-binding protein, and their enzymatic properties were examined. The reconstituted enzyme had ATP-dependent decatenation activity, which is the main catalytic activity of bacterial topoisomerase IV, and relaxing activities but had no supercoiling activity. So, the cloned genes were identified as P. aeruginosa topoisomerase IV genes. The inhibitory effects of quinolones on the activities of topoisomerase IV and DNA gyrase were compared. The 50% inhibitory concentrations of quinolones for the decatenation activity of topoisomerase IV were from five to eight times higher than those for the supercoiling activities of P. aeruginosa DNA gyrase. These results confirmed that topoisomerase IV is less sensitive to fluoroquinolones than is DNA gyrase and may be a secondary target of new quinolones in wild-type P. aeruginosa.  (+info)

(3/269) Impact of gyrA and parC mutations on quinolone resistance, doubling time, and supercoiling degree of Escherichia coli.

Isogenic mutants derived from quinolone-susceptible isolate WT by introducing gyrA (S83L, D87G) and parC (S80I, E84K) mutations associated with quinolone resistance were characterized with respect to quinolone resistance, growth rate, and degree of global supercoiling. The latter was determined by use of a pair of reporter plasmids carrying supercoiling-dependent promoters pgyrA and ptopA, respectively, transcriptionally fused to the reporter gene bla coding for TEM-1 beta-lactamase. The quotient (Qsc) of the beta-lactamase specific activity determined for a mutant carrying either plasmid was taken as a measure of the degree of global supercoiling. These Qsc data were comparable to results obtained from the separation of topoisomers of plasmid pBR322 on chloroquine-containing agarose gels and indicate a reduced degree of negative supercoiling in resistant mutants relative to the parent, WT. The S83L mutation in gyrA had the strongest influence on quinolone resistance while leaving other parameters nearly unaffected. The gyrA double mutation (S83L plus D87G) had an effect on quinolone resistance similar to that of a single mutation. Phenotypic expression of the parC mutation (S80I) was dependent on the presence of at least one gyrA mutation. Expression of high-level fluoroquinolone resistance (ciprofloxacin MIC, > 4 micrograms/ml) required a combination of the gyrA double mutation and one parC mutation (S80I or E84K). Such mutants showed considerable alterations of growth rate, global supercoiling, or both. Introduction of a parC mutation affected neither the doubling time nor the degree of supercoiling, while the presence of the gyrA D87G mutation was associated with a significant reduction in the degree of DNA supercoiling.  (+info)

(4/269) Penetration of moxifloxacin into peripheral compartments in humans.

To characterize the penetration of moxifloxacin (BAY 12-8039) into peripheral target sites, the present study aimed at measuring unbound moxifloxacin concentrations in the interstitial space fluid by means of microdialysis, an innovative clinical sampling technique. In addition, moxifloxacin concentrations were measured in cantharides-induced skin blisters, saliva, and capillary plasma and compared to total- and free-drug concentrations in venous plasma. For this purpose, 12 healthy volunteers received moxifloxacin in an open randomized crossover fashion either as a single oral dose of 400 mg or as a single intravenous infusion of 400 mg over 60 min. An almost-complete equilibration of the free unbound plasma fraction of moxifloxacin with the interstitial space fluid was observed, with mean area under the concentration-time curve (AUC)(interstitial fluid)/AUC(total-plasma) ratios ranging from 0.38 to 0.55 and mean AUC(interstitial fluid)/AUC(free-plasma) ratios ranging from 0.81 to 0.86. The skin blister concentration/plasma concentration ratio reached values above 1.5 after 24 h, indicating a preferential penetration of moxifloxacin into inflamed lesions. The moxifloxacin concentrations in saliva and capillary blood were similar to the corresponding levels in plasma. Our data show that moxifloxacin concentrations attained in the interstitial space fluid in humans and in skin blister fluid following single doses of 400 mg exceed the values for the MIC at which 90% of isolates are inhibited for most clinically relevant bacterial strains, notably including penicillin-resistant Streptococcus pneumoniae. These findings support the use of moxifloxacin for the treatment of soft tissue and respiratory tract infections in humans.  (+info)

(5/269) Pharmacokinetics of antibiotics in burn patients.

Drug pharmacokinetics are significantly altered in the burned patient but the interplay of a large number of variables is involved in deciding how an individual will deal with a drug. Consequently the burn patient population shows significant inter- and intrapatient variation. In 1976 altered aminoglycoside pharmacokinetics and the need for increased dosage in burn patients was reported but, despite this early study, a review of the currently available literature shows that for many drugs there is a paucity of information to support current dosage recommendations. In addition, many reports are based upon small numbers of patients, and even in larger studies there is no standardization of the study population with regard to the important variables known to affect drug handling. For the sub-population of burn patients who eliminate drugs extremely rapidly, a concern exists over the adequacy of antibiotic dosing. It is suggested that antibiotic serum concentrations be measured for all drugs in every patient to ascertain whether there is a significant problem with dosing. Additionally, future pharmacokinetic studies need to be standardized in burn patients.  (+info)

(6/269) Activity of moxifloxacin against mycobacteria.

Moxifloxacin is an 8-methoxyquinolone compound with activity against a wide range of bacteria. We tested its activity in comparison with four other quinolones and isoniazid against clinical isolates of mycobacteria. It proved to be the most active of the quinolones tested against Mycobacterium tuberculosis (MIC90 0.25 mg/L), Mycobacterium avium-intracellulare (MIC90 1.0 mg/L), Mycobacterium kansasii (MIC90 0.06 mg/L) and Mycobacterium fortuitum (MIC90 1 mg/L). These data indicate that moxifloxacin merits further study as an antimycobacterial agent.  (+info)

(7/269) Characterization of MexT, the regulator of the MexE-MexF-OprN multidrug efflux system of Pseudomonas aeruginosa.

We investigated the regulation of the MexEF-OprN multidrug efflux system of Pseudomonas aeruginosa, which is overexpressed in nfxC-type mutants and confers resistance to quinolones, chloramphenicol and trimethoprim. Sequencing of the DNA region upstream of the mexEF-oprN operon revealed the presence of an open reading frame (ORF) of 304 amino acids encoding a LysR-type transcriptional activator, termed MexT. By using T7-polymerase, a 34-kDa protein was expressed in Escherichia coli from a plasmid carrying the mexT gene. Expression of a mexE::lacZ fusion was 10-fold higher in nfxC-type mutants than in the wild-type strain; however, transcription of mexT as well as the mexT DNA region was unchanged. Located adjacent to mexT but transcribed in opposite direction, the beginning of an ORF termed qrh (quinone oxidoreductase homologue) was identified. Expression of a qrh::lacZ fusion was also found to be activated by MexT. Further, we present evidence for coregulation at the transcriptional and the posttranscriptional level between the MexEF-OprN efflux system and the OprD porin responsible for cross-resistance of nfxC-type mutants to carbapenem antibiotics.  (+info)

(8/269) Purification and inhibition by quinolones of DNA gyrases from Mycobacterium avium, Mycobacterium smegmatis and Mycobacterium fortuitum bv. peregrinum.

The DNA gyrases from Mycobacterium avium, Mycobacterium smegmatis and Mycobacterium fortuitum bv. peregrinum, which are species naturally resistant, moderately susceptible and susceptible to fluoroquinolones, respectively, were purified by affinity chromatography on novobiocin-Sepharose columns. The DNA gyrase inhibiting activities (IC50 values) of classical quinolones and fluoroquinolones were determined from the purified enzymes and were compared to the corresponding antibacterial activities (MICs). Regarding M. fortuitum bv. peregrinum, which is nearly as susceptible as Escherichia coli, the corresponding MIC and IC50 values of quinolones were significantly lower than those found for M. avium and M. smegmatis (e.g. for ofloxacin, MICs of 0.25 versus 32 and 1 microg ml(-1), and IC50 values of 1 versus 8 and 6 microg ml(-1), respectively). Such a result could be related to the presence of Ser-83 in the quinolone-resistance-determining region of the gyrase A subunit of M. fortuitum bv. peregrinum, as found in wild-type E. coli, instead of Ala-83 in M. avium and M. smegmatis, as found in fluoroquinolone-resistant E. coli mutants. The IC50 values of quinolones against the M. avium and M. smegmatis DNA gyrases were similar, while the corresponding MICs were 32-fold higher for M. avium when compared to M. smegmatis, suggesting that an additional mechanism, such as a low cell wall permeability or a drug efflux, could contribute to the low antibacterial potency of quinolones against M. avium.  (+info)

*  4-Quinolone
It and 2-quinolone are the two most important parent (meaning simplified) quinolones. 4-Quinolone exists in equilibrium with a ... The hydroxyquinolines tautomerize to the quinolones. Andriole, VT The Quinolones. Academic Press, 1989. Shi, Pengfei; Wang, ... The chemical synthesis of quinolones often involves ring-closing reactions. Such reactions often install a hydroxyl group (an - ... Lili; Chen, Kehao; Wang, Jie; Zhu, Jin (2017). "Co(III)-Catalyzed Enaminone-Directed C-H Amidation for Quinolone Synthesis". ...
*  Flumequine
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 ...
*  Norfloxacin
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. ...
*  Ofloxacin
quinolones for community-acquired pneumonia: meta-analysis of randomized controlled trials". Clin. Microbiol. Infect. 19 (4): ... Research and Development of Quinolones in Daiichi Sankyo Co., Ltd. Archived 2016-10-12 at the Wayback Machine. Page accessed ... Simultaneous use of corticosteroids is present in almost one-third of quinolone-associated tendon rupture. Tendon damage may ... Jones SF, Smith RH (March 1997). "Quinolones may induce hepatitis". BMJ. 314 (7084): 869. doi:10.1136/bmj.314.7084.869. PMC ...
*  Pefloxacin
... is a quinolone antibiotic used to treat bacterial infections. Pefloxacin has not been approved for use in the United ... Casparian JM, Luchi M, Moffat RE, Hinthorn D (May 2000). "Quinolones and tendon ruptures". South. Med. J. 93 (5): 488-91. doi: ... and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377-92. PMC 232616 . PMID 9293187. Khaliq Y, Zhanel GG (October 2005). " ... 32 (4): 495-502, vi. doi:10.1016/j.cps.2005.05.004. PMID 16139623. ...
*  Fleroxacin
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 ...
*  Cinoxacin
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 ...
*  Moxifloxacin
Peterson, U. (2006). "Quinolone Antibiotics: The Development of Moxifloxacin". In IUPAC; Fischer, J.; Ganellin, C. R. Analogue- ... any member of the quinolone class of antimicrobial agents, or any of the product components." Though not stated as such within ... Drlica K, Zhao X (1 September 1997). "DNA gyrase, topoisomerase IV, and the 4-quinolones". Microbiol Mol Biol Rev. 61 (3): 377- ... 4% of an oral dose is excreted as either unchanged drug or known metabolites. The mean (± SD) apparent total body clearance and ...
*  Levofloxacin
Like all quinolones, it functions by inhibiting the DNA gyrase and topoisomerase IV. Topoisomerase IV is necessary to separate ... Research and Development of Quinolones in Daiichi Sankyo Co., Ltd. Archived 12 October 2016 at the Wayback Machine. Page ... Lafredo SC, Foleno BD, Fu KP (1993). "Induction of resistance of Streptococcus pneumoniae to quinolones in vitro". Chemotherapy ... Levofloxacin is the levo isomer of the racemate ofloxacin, another quinolone antimicrobial agent. Levofloxacin, a chiral ...
*  2-Quinolone
... is an organic compound related structurally to quinoline. It is the majority tautomer in equilibrium with 2- ... The isomer 4-quinolone is the parent of a large class of quinolone antibiotics. Tashima, Toshihiko (2015). "The structural use ...
*  SER-601
... (COR-167) is a drug which acts as a potent and selective cannabinoid CB2 receptor agonist, based on a quinolone-3- ... August 2008). "Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of ... August 2010). "Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and ... pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands ...
*  ELQ-300
2013). "Quinolone-3-diarylethers: a new class of antimalarial drug". Science Translational Medicine. 5 (177): 177ra37. doi: ... It is the first entry in a new class of antimalarials known as 4-quinolone-3-diarylethers. ELQ-300 acts as an inhibitor of the ...
*  GABAA receptor
140 (4): 403-5. doi:10.1007/s10517-005-0503-z. PMID 16671565. He, Y.; Benz, A.; Fu, T.; Wang, M.; Covey, D.F.; Zorumski, C.F.; ... 67 (4): 310-8. doi:10.1016/j.brainresbull.2005.07.004. PMID 16182939. Yarom, M.; Tang, X. W.; Wu, E.; Carlson, R. G.; Vander ... 4 (5): 759-65. doi:10.1016/0896-6273(90)90202-Q. PMID 2160838. ; (j) Majewska MD, Harrison NL, Schwartz RD, Barker JL, Paul SM ... 5 (4): 274-280. ISSN 1021-7770. PMID 9691220. Cossart R, Bernard C, Ben-Ari Y (2005). "Multiple facets of GABAergic neurons and ...
*  Amfonelic acid
20 (4): 635-7. doi:10.1016/0091-3057(84)90316-2. PMID 6728880. Pu, C; Fisher, JE; Cappon, GD; Vorhees, CV (1994). "The effects ... In 1988 the biologist G.C. Crumplin wrote, "[AFA] is less active against bacteria than are many other 4-quinolones, but studies ... Crumplin, G.C. (1988). "Aspects of Chemistry in the Development of the 4-Quinolone Antibacterial Agents". Reviews of Infectious ... 4-dihydroxyphenylacetic acid concentration in spiperone-treated rats". Journal of Pharmacy and Pharmacology. 30 (3): 197-198. ...
*  Antibiotic resistance in gonorrhea
If there is a mutation in the DNA gyrase, then the quinolone will not be able to bind to it resulting in the activity of DNA ... Low-level quinolone resistance has been linked to changes in cell permeability and efflux pumps. The NorM efflux pump is ... Second generation quinolones like ciprofloxacin and ofloxacin have been widely used to treat N. gonorrhoeae infections. ... The plasmids containing TEM-1 could be passed from bacterium to bacterium via conjugation Quinolones are a class of synthetic ...
*  Autoinducer
1999). "). Quinolone signaling in the cell-to-cell communication system of Pseudomonas aeruginosa". Proc. Natl. Acad. Sci. USA ... 43 (4): 496-518. PMC 281490 . PMID 396467. Churchill, M.E.; Chen, L. (2011). "Structural basis of acyl-homoserine lactone- ... 181 (4): 1203-1210. PMC 93498 . PMID 9973347. Fuqua, C.; Winans, S.C. (1996). "Conserved cis-acting promoter elements are ... P. aeruginosa also uses 2-heptyl-3-hydroxy-4-quinolone (PQS) for quorum sensing. This molecule is noteworthy because it does ...
*  Galangin
Cushnie TP, Lamb AJ (2006). "Assessment of the antibacterial activity of galangin against 4-quinolone resistant strains of ...
*  Ullmann condensation
A Two-Step Synthesis of 2-Aryl-4-quinolones from o-Halophenones". J. Org. Chem. 72 (21): 7968-7973. doi:10.1021/jo701384n. PMID ...
*  Quinolone antibiotic
... at Curlie (based on DMOZ) Healthcare-associated Infections (HAIs)- Quinolones and the Clinical Laboratory ... Although not formally a quinolone, nalidixic acid is considered the first quinolone drug. It was introduced in 1962 for ... Norris, S; Mandell, GL (1988). "The quinolones: history and overview". The quinolones: history and overview. San Diego: ... VT The Quinolones. Academic Press, 1989. Andersson MI, MacGowan AP (2003). "Development of the quinolones". Journal of ...
*  Camps quinoline synthesis
... making the compound a quinolone. An example of the Camps reaction is given below: Camps, R.; Ber. 1899, 22, 3228. Camps, R.; ... Review) Sequential Cu-Catalyzed Amidation-Base-Mediated Camps Cyclization: A Two-Step Synthesis of 2-Aryl-4-quinolones from o- ...
*  Conrad-Limpach synthesis
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 ... for the quinolone CP-115,953 in yeast". J Biol Chem. 267 (19): 13150-3. PMID 1320012. ^ Baba, A., et al. Studies on Disease- ... Brouet, J.C., Gu, S., Peet, N.P., Williams, J.D. A Survey of Solvents for the Conrad-Limpach Synthesis of 4-Hydroxyquinolones ( ...
*  Pseudoalteromonas piscicida
45 (4): 755-761. doi:10.1099/00207713-45-4-755. ISSN 0020-7713. "Kristen Whalen , Haverford College". www.haverford.edu. ... It is known to produce a quorum sensing molecule called 2-heptyl-4-quinolone (HHQ), which functions as a bacterial infochemical ...
*  List of MeSH codes (D03)
... quinolones MeSH D03.438.810.835.055 --- 4-quinolones MeSH D03.438.810.835.055.500 --- nalidixic acid MeSH D03.438.810.835. ... 4,5-tetrahydro-8-chloro-3-methyl-5-phenyl-1h-3-benzazepin-7-ol MeSH D03.438.079.800 --- 2,3,4,5-tetrahydro-7,8-dihydroxy-1- ... 4,5-dihydro-1-(3-(trifluoromethyl)phenyl)-1h-pyrazol-3-amine MeSH D03.383.129.539.200 --- epirizole MeSH D03.383.129.539.487 ... 4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, methyl ester MeSH D03.383.725.210 --- dimethindene MeSH D03.383. ...
*  Leonard Klevan
... and the 4-quinolones". Microbiol. Mol. Biol. Rev. 61 (3): 377-92. September 1997. PMC 232616 . PMID 9293187. "Novel ...
*  Furoquinoline alkaloid
One furoquinoline alkaloid, 5-(1,1-dimethylallyl)-8-hydroxy-furo[2-3-b]quinolone, shows antifungal properties against ... 8-trimethoxy-2-quinolone from hydrolysis. Some furoquinoline alkaloids have been found to have in vitro pharmacological ... 4 (6): 399-404. PMID 22491304. Cardoso-Lopes, Elaine Monteiro; Maier, James Andreas; Silva, Marcelo Rogério da; Regasini, Luis ... Aromatic methoxy group give responses in 4.0-4.2 ppm region but 4-methoxy group give responses in ~4.40 ppm region. Cordell, ...
*  New Delhi metallo-beta-lactamase 1
As previously, the bacteria were fully resistant to all the aminoglycoside β-lactam and quinolone antibiotics, but were ... 9 (4): 228-236. doi:10.1016/S1473-3099(09)70054-4. PMID 19324295. Cuzon G, Naas T, Nordmann P (February 2010). "KPC ... 4 August 2010). "Type IIA topoisomerase inhibition by a new class of antibacterial agents". Nature. 466 (7309): 935-940. doi: ... Yi Luo, Fenxia Yang, Jacques Mathieu, Daqing Mao, Qing Wang, and P.J.J. Alvarez (December 4, 2013), Proliferation of Multidrug- ...
4-Quinolone - Wikipedia  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 chemical synthesis of quinolones often involves ring-closing reactions. Such reactions often install a hydroxyl group (an - ... Lili; Chen, Kehao; Wang, Jie; Zhu, Jin (2017). "Co(III)-Catalyzed Enaminone-Directed C-H Amidation for Quinolone Synthesis". ...
more infohttps://en.wikipedia.org/wiki/4-Quinolone
4-Quinolone-3-Carboxamide CB2 Ligand- CAS Number 1314230-69-7  4-Quinolone-3-Carboxamide CB2 Ligand- CAS Number 1314230-69-7
Buy 4-Quinolone-3-Carboxamide CB2 Ligand - CAS Number 1314230-69-7 from LGC Standards. Please login or register to view prices ...
more infohttps://www.lgcstandards.com/FR/en/4-Quinolone-3-Carboxamide-CB2-Ligand/p/CAY-11093-1MG
4-Quinolone-3-Carboxamide CB2 Ligand- CAS Number 1314230-69-7  4-Quinolone-3-Carboxamide CB2 Ligand- CAS Number 1314230-69-7
Buy 4-Quinolone-3-Carboxamide CB2 Ligand - CAS Number 1314230-69-7 from LGC Standards. Please login or register to view prices ...
more infohttps://www.lgcstandards.com/FR/en/4-Quinolone-3-Carboxamide-CB2-Ligand/p/CAY-11093-10MG
The Pseudomonas aeruginosa PrrF1 and PrrF2 Small Regulatory RNAs Promote 2-Alkyl-4-Quinolone Production through Redundant...  The Pseudomonas aeruginosa PrrF1 and PrrF2 Small Regulatory RNAs Promote 2-Alkyl-4-Quinolone Production through Redundant...
4. (. [. a. n. t. R. ]. o. ×. [. PrrF. ]. ). 2. ×. [. a. n. t. R. ]. o. (3) where KDR is the dissociation constant for the antR ... Two distinct pathways supply anthranilate as a precursor of the Pseudomonas quinolone signal. J Bacteriol 189:3425-3433. doi: ... These AQs include the Pseudomonas quinolone signal (PQS) and 2-heptyl-4-hydroxyquinolone (HHQ) quorum-sensing molecules, which ... Interference with Pseudomonas quinolone signal synthesis inhibits virulence factor expression by Pseudomonas aeruginosa. Proc ...
more infohttps://jb.asm.org/content/200/10/e00704-17
A Mild and Efficient Synthesis of 4-Quinolones and Quinolone Heterocycles  A Mild and Efficient Synthesis of 4-Quinolones and Quinolone Heterocycles
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1-hydroxy-2-dodecyl-4(1H)quinolone | C21H31NO2 - PubChem  1-hydroxy-2-dodecyl-4(1H)quinolone | C21H31NO2 - PubChem
... quinolone , C21H31NO2 , CID 600305 - structure, chemical names, physical and chemical properties, classification, patents, ...
more infohttps://pubchem.ncbi.nlm.nih.gov/compound/600305
ChemIDplus - 112182-50-0 - QKTGFMIEELHDSD-UHFFFAOYSA-N - 6-Chloro-2-phenyl-4-quinolone - Similar structures search, synonyms,...  ChemIDplus - 112182-50-0 - QKTGFMIEELHDSD-UHFFFAOYSA-N - 6-Chloro-2-phenyl-4-quinolone - Similar structures search, synonyms,...
6-Chloro-2-phenyl-4-quinolone - Similar structures search, synonyms, formulas, resource links, and other chemical information. ... Substance Name: 6-Chloro-2-phenyl-4-quinolone. RN: 112182-50-0. InChIKey: QKTGFMIEELHDSD-UHFFFAOYSA-N. Note. *. Interacts with ... 1S/C15H10ClNO/c16-11-6-7-13-12(8-11)15(18)9-14(17-13)10-4-2-1-3-5-10/h1-9H,(H,17,18). Download. ...
more infohttps://chem.nlm.nih.gov/chemidplus/rn/112182-50-0
Pharmaceutical Chemicals - Market Size, Market Share, Market Leaders, Demand Forecast, Sales, Company Profiles, Market Research...  Pharmaceutical Chemicals - Market Size, Market Share, Market Leaders, Demand Forecast, Sales, Company Profiles, Market Research...
US demand for pharmaceutical chemicals will rise 6.5 percent annually to $46.9 billion in 2019. Hormones will be the fastest growing products, led by active ingredients of anticancer, antidiabetic, and hormone replacement formulations. Central nervous system chemicals will remain the largest segment, and will be the second fastest growing.This study analyzes the $34.2 billion US pharmaceutical chemical industry. It presents historical demand data (2004, 2009 and 2014) and forecasts (2019 and 2024) by chemical type (e.g., central nervous system, hormones and related, cardiovascular, anti-infective, nutritional, biological, respiratory, gastrointestinal, dermatological).The study also considers market environment factors, details industry structure, evaluates company market share, and profiles 31 industry participants, including Teva Pharmaceutical Industries, Royal DSM, and Aurobindo Pharma.
more infohttps://www.freedoniagroup.com/industry-study/pharmaceutical-chemicals-3280.htm
The Toxoplasma Blog: Genetic Evidence for Cytochrome b Qi Site Inhibition by 4(1H)-quinolone-3-diarylethers and Antimycin in...  The Toxoplasma Blog: Genetic Evidence for Cytochrome b Qi Site Inhibition by 4(1H)-quinolone-3-diarylethers and Antimycin in...
Endochin-like-quinolones (ELQs) are preclinical compounds that are efficacious against apicomplexan-caused diseases including ... Alday PH1, Bruzual I2, Nilsen A2, Pou S2, Winter R2, Ben Mamoun C3, Riscoe MK2, Doggett JS4,2. ... Genetic Evidence for Cytochrome b Qi Site Inhibition by 4(1H)-quinolone-3-diarylethers and Antimycin in Toxoplasma gondii ...
more infohttp://toxoplasmaparasite.blogspot.com/2016/12/genetic-evidence-for-cytochrome-b-qi.html
Relationship between effective lens position and axial position of a thick intraocular lens.  Relationship between effective lens position and axial position of a thick intraocular lens.
QUINOLONES containing a 4-oxo (a carbonyl in the para position to the nitrogen). They inhibit the A subunit of DNA GYRASE and ... Second generation 4-quinolones are also substituted with a 1-piperazinyl group at the 7-position and a fluorine at the 6- ...
more infohttps://www.bioportfolio.com/resources/pmarticle/2070606/Relationship-between-effective-lens-position-and-axial-position-of-a-thick-intraocular.html
antibiotic resistance Flashcards by Isabel Leach | Brainscape  antibiotic resistance Flashcards by Isabel Leach | Brainscape
Quinolone resistance by mutating binding site. A subunit of DNA gyrase, coded by gyrA has lowered affinity. ...
more infohttps://www.brainscape.com/flashcards/antibiotic-resistance-3697320/packs/5494219
Yerba Mate: Uses, Side Effects, Interactions, Dosage, and Warning  Yerba Mate: Uses, Side Effects, Interactions, Dosage, and Warning
Antibiotics (Quinolone antibiotics) interacts with YERBA MATE. The body breaks down caffeine to get rid of it. Some antibiotics ... Effect of quinolones on caffeine disposition. Clin Pharmacol Ther 1989;45:234-40. View abstract. ... 2011;12(4):1089-93. View abstract.. *Stille, W., Harder, S., Mieke, S., Beer, C., Shah, P. M., Frech, K., and Staib, A. H. ... 1999;6(4):231-238. View abstract.. *Martins, F., Noso, T. M., Porto, V. B., Curiel, A., Gambero, A., Bastos, D. H., Ribeiro, M ...
more infohttps://www.webmd.com/vitamins/ai/ingredientmono-828/yerba-mate
Category:Quinolones - Wikimedia Commons  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 ... quinolones (en); chinolony (pl); Kinoloner (nb); Quinolone, Quinolon, Quinolonen, Chinolonen (nl) ... Media in category "Quinolones". The following 35 files are in this category, out of 35 total. ...
more infohttps://commons.wikimedia.org/wiki/Category:Quinolones
Nedocromil
      - Alocril
     Summary Report | CureHunter  Nedocromil - Alocril Summary Report | CureHunter
4. Cough 03/01/1988 - "Nedocromil sodium may prove useful in the treatment of unproductive cough in situations where the use of ... Alocril; Tilade; 9-Ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyrano(3,2-g)quinoline-2,8-dicarboxylic acid; ASTA Medica Brand of ... in adult patients of up to 52 weeks duration have demonstrated the tolerability and efficacy of nedocromil 4 mg twice or 4 ...
more infohttp://www.curehunter.com/public/keywordSummaryD017835-Nedocromil-Alocril.do
Antibiotic treatment enhances the genome-wide mutation rate of target cells | PNAS  Antibiotic treatment enhances the genome-wide mutation rate of target cells | PNAS
1990) Quinolone resistance-determining region in the DNA gyrase gyrA gene of Escherichia coli. Antimicrob Agents Chemother 34(6 ... 1989) Mechanism of inhibition of DNA gyrase by quinolone antibacterials: A cooperative drug-DNA binding model. Biochemistry 28( ... are not in known quinolone resistance determining regions (QRDRs) (62), and they thus reveal a larger mutational space of the ... 4). Notably, two MMR− lines (SA6 and SA12; Dataset S1, Table S5) grown in the absence of norfloxacin exhibited a ≥2 times ...
more infohttps://www.pnas.org/content/113/18/E2498
DIAMORPHINE HYDROCHLORIDE BP 30MG LYOPHILISATE FOR SOLUTION FOR INJECTION | Drugs.com  DIAMORPHINE HYDROCHLORIDE BP 30MG LYOPHILISATE FOR SOLUTION FOR INJECTION | Drugs.com
4.. 8.5 pt. 5.. 6.. Technical Approval. date sent:. revised by:. supplier:. min pt size:. colours/plates:. approved:. 5.2.16. ... 4.. 8.5 pt. 5.. 6.. Technical Approval. date sent:. revised by:. supplier:. min pt size:. colours/plates:. approved:. 5.2.16. ... To relieve pain 5 - 10 mg every 4. hours injected under the skin or into a. muscle.. If the drug is given directly into a vein, ... An antibiotic called 4-quinolone. • Cimetidine, used to treat stomach. ulcers and indigestion, or if. • You have been drinking ...
more infohttps://www.drugs.com/uk/diamorphine-hydrochloride-bp-30mg-lyophilisate-for-solution-for-injection-leaflet.html
The Influence of Antibiotics on the Host-Parasite Relationship III | Günther Gillissen | Springer  The Influence of Antibiotics on the Host-Parasite Relationship III | Günther Gillissen | Springer
Effect of 4-Quinolone Antibiotics on Cell Function, Cell Growth, and Pyrimidine Nucleotide Biosynthesis in Human Lymphocytes In ... With 2 Figures and 5 Tables . . . . . . .. 4 Influence of Antibiotics on the Cell Surface of Escherichia coli H. Leying, S. ... With 2 Figures and 3 Tables . . . . . 17 Pseudomonas aeruginosa: Alterations Induced by Low Concentrations of 4-Quinolones M. T ...
more infohttps://www.springer.com/us/book/9783642736551?wt_mc=
Preparation and evaluation of danofloxacin mesylate microspheres and its pharmacokinetics in pigs | SpringerLink  Preparation and evaluation of danofloxacin mesylate microspheres and its pharmacokinetics in pigs | SpringerLink
Hannan, P.C.T., Hanlon, P.J.O. & Rogers, N.M. (1989). In vitro evaluation of various quinolone antibacterial agents against ... Neu, H.C. (1991). Synergy and antagonism of combinations with quinolones. European journal of clinical microbiology and ... Drlica, K. & Zhao, X. (1997). DNA gyrase, topoisomerase i.v. and the 4-quinolones. Microbiology and Molecular Biology Reviews ...
more infohttps://link.springer.com/article/10.1007%2Fs11259-009-9320-6
Quorum Sensing | SpringerLink  Quorum Sensing | SpringerLink
Quantifying Pseudomonas aeruginosa Quinolones and Examining Their Interactions with Lipids Gregory C. Palmer, Jeffrey W. ... Liquid Chromatography/Mass Spectrometry for the Detection and Quantification of N-Acyl-l-Homoserine Lactones and 4-Hydroxy-2- ...
more infohttps://link.springer.com/book/10.1007%2F978-1-60761-971-0
  • Endochin-like-quinolones (ELQs) are preclinical compounds that are efficacious against apicomplexan-caused diseases including toxoplasmosis, malaria and babesiosis. (blogspot.com)
  • We further characterized resistant strains selected with the combination of ciprofloxacin and WCK-1734 and found evidence to suggest the existence of novel mutational mechanisms for low-level quinolone resistance. (asm.org)
  • Quinolones act by forming ternary complexes with DNA and either DNA gyrase or TopoIV, thereby blocking DNA replication and triggering events leading to cell death ( 5 , 12 ). (asm.org)
  • In 2008, the United States Food and Drug Administration (FDA) requested that all quinolone/fluoroquinolone drugs package inserts include a Black Boxed Warning concerning the risk of spontaneous tendon ruptures, which would have included flumequine. (wikipedia.org)
  • P. aeruginosa virulence depends on a multitude of virulence factors that include exotoxins ( 1 - 3 ), cell-to-cell communication via quorum-sensing factors ( 4 - 6 ), and nutrient acquisition systems ( 7 ). (asm.org)
  • Recent studies have demonstrated a correlation between mammalian cell cytotoxicity of the quinolones and the induction of micronuclei. (wikipedia.org)
  • However, PCD has also been found in unicellular eukaryotes ( 4 ) and even in prokaryotes ( 19 , 23 , 28 , 42 ). (asm.org)
  • We first determined by genetic and biochemical studies in Staphylococcus aureus that the primary target enzyme of WCK-1734, a new quinolone, was DNA gyrase. (asm.org)
  • 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)
  • The PrrF sRNAs promote the production of 2-akyl-4(1 H )-quinolone metabolites (AQs) that mediate a range of biological activities, including quorum sensing and polymicrobial interactions. (asm.org)
  • Such reactions often install a hydroxyl group (an -OH functional group on the carbon across from the ring nitrogen (i.e., the C-4 positions). (wikipedia.org)
  • Second generation 4-quinolones are also substituted with a 1-piperazinyl group at the 7-position and a fluorine at the 6-position. (bioportfolio.com)