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Quinolones

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https://www.readbyqxmd.com/read/29332148/occurrence-of-pharmaceuticals-and-personal-care-products-and-their-associated-environmental-risks-in-a-large-shallow-lake-in-north-china
#1
Panwei Zhang, Huaidong Zhou, Kun Li, Xiaohui Zhao, Qiaona Liu, Dongjiao Li, Gaofeng Zhao
Eighteen selected pharmaceuticals and personal care products (PPCPs), consisting of five non-antibiotic pharmaceuticals (N-APs), four sulfonamides (SAs), four tetracyclines (TCs), four macrolides (MCs), and one quinolone (QN) were detected in water, pore water, and sediment samples from Baiyangdian Lake, China. A total of 31 water samples and 29 sediment samples were collected in March 2017. Caffeine was detected with 100% frequency in surface water, pore water, and sediment samples. Carbamazepine was detected with 100% frequency in surface water and sediment samples...
January 13, 2018: Environmental Geochemistry and Health
https://www.readbyqxmd.com/read/29327005/vivo-complexes-with-antibacterial-quinolone-ligands-and-their-interaction-with-serum-proteins
#2
Daniele Sanna, Valeria Ugone, Giuseppe Sciortino, Péter Buglyó, Zsolt Bihari, Péter László Parajdi-Losonczi, Eugenio Garribba
Quinolone derivatives are among the most commonly prescribed antibacterials in the world and could also attract interest as organic ligands in the design of metal complexes with potential pharmacological activity. In this study, five compounds, belonging to the first (nalidixic acid or Hnal), second (ciprofloxacin or Hcip, and norfloxacin or Hnor) and third generation (levofloxacin or Hlev, and sparfloxacin or Hspar) of quinolones, were used as ligands to bind the VIVO2+ ion. In aqueous solution, mono- and bis-chelated species were formed as a function of pH, with cis-[VOHxL2(H2O)]x+ and [VOHxL2]x+, x = 0-2, being the major complexes at pH 7...
January 12, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29323495/cascade-reaction-of-isatins-with-1-1-enediamines-synthesis-of-multisubstituted-quinoline-4-carboxamides
#3
Bao-Qu Wang, Cong-Hai Zhang, Xiao-Xue Tian, Jun Lin, Sheng-Jiao Yan
A one-step methodology for the synthesis of multisubstituted quinoline-4-carboxamides was developed by simply refluxing a mixture of isatins 1 and various kinds of 1,1-enediamines 2-4 in a reaction catalyzed by NH2SO3H. As a result, a series of quinolone-4-carboxamides were produced through a novel cascade reaction mechanism. This reaction involved the formation of the quinoline ring accompanied by the formation of an amide bond in one step. Accordingly, this protocol is suitable for combinatorial and parallel syntheses of quinolone-4-carboxamide drugs or natural products...
January 11, 2018: Organic Letters
https://www.readbyqxmd.com/read/29322454/methods-for-measuring-the-production-of-quorum-sensing-signal-molecules
#4
Manuel Alcalde-Rico, José Luis Martínez
One relevant aspect for understanding the bottlenecks that modulate the spread of resistance among bacterial pathogens consists in the effect that the acquisition of resistance may have on the microbial physiology . Whereas studies on the effect of acquiring resistance of bacterial growth are frequently performed, more detailed analyses aiming to understand in depth the cross talk between resistance and virulence, including bacterial communication are less frequent. The bacterial quorum sensing system, is an important intraspecific and interspecific communication system highly relevant for many physiological processes, including virulence and bacterial/host interactions...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29321384/discovery-of-a-novel-fluoroquinolone-antibiotic-candidate-wfq-228-with-potent-antimicrobial-activity-and-the-potential-to-overcome-major-drug-resistance
#5
Tatsuya Hirano, Tomohiko Kinoshita, Daichi Kazamori, Satoshi Inoue, Kouji Nishimura, Asuka Sakurai, Kensuke Ohishi, Yasuhiro Kuramoto, Hirotaka Amano, Akira Yazaki
WFQ-101 with a unique N-1 substituent, 5-amino-4-fluoro-2-(hydroxymethyl)phenyl group, was selected as a lead compound through combination screening based on antimicrobial activity and the efflux index against quinolone-resistant (QR) Pseudomonas aeruginosa (P. aeruginosa). Through structural optimization, we identified WFQ-228 as a novel fluoroquinolone antibiotic candidate. WFQ-228 had potent and superior activity in comparison to levofloxacin (LVX) and ciprofloxacin (CIP) against clinical isolates of P. aeruginosa, Escherichia coli and Acinetobacter baumannii, including QR strains...
January 11, 2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29319519/analyses-of-plasmids-harbouring-quinolone-resistance-determinants-in-enterobacteriaceae-members
#6
Bayri Erac, Fethiye Ferda Yilmaz, Ismail Ozturk, Sabire Sohret Aydemir, Mine Hosgor-Limoncu
The aim of this study was to explore the plasmid characteristics of eight clinical Enterobacteriaceae strains containing extended broad spectrum beta-lactamases and plasmid-mediated quinolone resistance. Plasmids were transferred by conjugation or transformation and resistance determinants were investigated by PCR. We showed that at least one plasmid harbouring qnrB or qnrS determinant was transferred by conjugation in five isolates. QepA determinant was confirmed to be on a non-conjugative plasmid. We found at least one beta-lactamase gene in seven of the eight clinical isolates having plasmid-mediated quinolone resistance, which indicated that these two resistance determinants were mostly on the same conjugative plasmids...
December 4, 2017: Polish Journal of Microbiology
https://www.readbyqxmd.com/read/29319210/the-safety-of-quinolones-and-fluoroquinolones-in-pregnancy-a-meta-analysis
#7
Enav Yefet, Naama Schwartz, Bibiana Chazan, Raed Salim, Shabtai Romano, Zohar Nachum
BACKGROUND: Quinolones were contraindicated during pregnancy due to concerns regarding fetal malformations and carcinogenesis in animals. The literature is conflicted regarding their safety in humans. OBJECTIVES: To conducted a meta-analysis evaluating the risk for fetal malformations and pregnancy complications following exposure to quinolones during pregnancy. SEARCH STRATEGY: We searched Embase, PubMed, Medline, the Cochrane database, clinicaltrials...
January 10, 2018: BJOG: An International Journal of Obstetrics and Gynaecology
https://www.readbyqxmd.com/read/29317251/organoselenium-group-is-critical-for-antioxidant-activity-of-7-chloro-4-phenylselenyl-quinoline
#8
Ane G Vogt, Guilherme T Voss, Renata L de Oliveira, Jaini J Paltian, Luis F B Duarte, Diego Alves, Cristiano R Jesse, Silvane S Roman, Juliano A Roehrs, Ethel A Wilhelm, Cristiane Luchese
The quinolone compounds have been reported for many biological properties, especially as potent antioxidants. This study investigated the antioxidant effect of 7-chloro-4-phenylselenyl-quinoline (PSQ), a quinolone derivative with organoselenium group, against oxidative stress induced by sodium nitroprusside (SNP) in brains of mice. A second objective was to verify the importance of phenylselenyl group presents at position 4 of the quinoline structure to antioxidant effect of compound. So, it was compared the antioxidant effect of PSQ with a quinoline without organoseleniun group (7-chloroquinoline [QN])...
January 6, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29316136/transrectal-prostate-biopsy-sepsis-rate-following-reduced-quinolone-antibiotic-prophylaxis-from-six-doses-to-single-dose
#9
Haider K Bangash, Cynthia Hawks, Steve P McCombie, Matthew Brown, Dickon Hayne
BACKGROUND: This study aimed to evaluate the rates of infective complication related to transrectal prostate biopsy (TRPB) as our centre changed its protocol from six doses over 3 days to a single pre-procedure prophylactic dose. METHODS: This prospective cohort study identified infective complication in patients who attended and subsequently underwent TRPB at the time of their one-stop prostate clinic at our public tertiary hospital between August 2011 and April 2017...
January 8, 2018: ANZ Journal of Surgery
https://www.readbyqxmd.com/read/29313868/pets-as-potential-carriers-of-multidrug-resistant-enterococcus-faecium-of-significance-to-public-health
#10
Giorgia Dotto, Michele Berlanda, Daniela Pasotto, Alessandra Mondin, Giorgio Zambotto, Maria Luisa Menandro
Enterococci are important opportunistic pathogens for humans and animals and have recently become one of the leading causes of nosocomial infections, raising concerns about their virulence and antimicrobial traits. This study describes a multidrug-resistant Enterococcus faecium isolated from a case of feline urinary tract infection. This strain was characterized for virulence and antimicrobial resistance markers, phylogenetic group and sensitivity to antimicrobial agents used routinely in veterinary and human practice...
January 9, 2018: New Microbiologica
https://www.readbyqxmd.com/read/29308712/in-silico-approaches-illustrate-the-evolutionary-pattern-and-protein-small-molecule-interactions-of-quinolone-synthase-from-aegle-marmelos-correa
#11
Mallika Vijayanathan, K C Sivakumar, Aiswarya Girija, E V Soniya
Quinolone synthase from Aegle marmelos (AmQNS) is a Rutacean-specific plant type III polyketide synthase that synthesizes quinolone, acridone and benzalacetone with therapeutic potential. Simple architecture and broad substrate affinity of AmQNS make it as one of the target enzymes to produce novel structural scaffolds. Another unique feature of AmQNS despite its high similarity to acridone forming type III polyketide synthase from Citrus microcarpa is the variation in the product formation. Hence, to explore the characteristic features of AmQNS, an in-depth sequence and structure-based bioinformatics analyses were performed...
January 8, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29307860/high-frequency-of-the-aac-6-ib-cr-gene-associated-with-double-mutations-in-gyra-and-parc-in-escherichia-coli-isolates-from-patients-with-urinary-tract-infections
#12
Lisiane M Volcão, Juliano P Lacava, Martina F Gewehr, Valéria L Real, Ivy B Ramis, Daniela F Ramos, Carla V Gonçalves, Lia G Possuelo, Luciene A R Minarini, Pedro E A da Silva, Andrea von Groll
OBJECTIVE: The aims of this study were (1) to determine the frequency of plasmid-mediated resistance to fluoroquinolones (FQs) in Escherichia coli isolated from patients with urinary tract infections (UTIs) of nosocomial and community origin and (2) to determine the relationships between the presence of extended spectrum beta lactamases (ESBL), mutations in the gyrA and parC genes, and resistance to FQs. METHODS: A total of 71 E. coli isolates, including 35 ESBL producers and 36 randomly selected non-ESBL-producers, were analysed...
January 4, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29303546/establishment-of-lcms-based-platform-for-discovery-of-quorum-sensing-inhibitors-signal-detection-in-pseudomonas-aeruginosa-pao1
#13
Manoj Kushwaha, Shreyans K Jain, Nisha Sharma, Vidushi Abrol, Sundeep Jaglan, Ram A Vishwakarma
Targeting the main three networking systems viz. Las, RhI and PQS via natural quenchers is a new ray of hope for combating the persistent behavior of Pseudomonas aeruginosa. In the bacterial chemical vocabulary pyocyanin, N-AHLs and rhamnolipids are the main keywords, which are responsible for the social and nomadic behavior of P. aeruginosa. In the present work LCMS-based real-time qualitative and quantitative analysis of pyocyanin, green phenazine, N-AHLs, and rhamnolipids were performed. The quantitative analysis indicates that the production of pyocyanin and NHSLs increases with time while the production of rhamnolipids discontinued after 16 Hrs...
January 5, 2018: ACS Chemical Biology
https://www.readbyqxmd.com/read/29300775/analytical-profiling-of-mutations-in-quinolone-resistance-determining-region-of-gyra-gene-among-upec
#14
Lesley R Varughese, Meenakshi Rajpoot, Soniya Goyal, Ravinder Mehra, Vinod Chhokar, Vikas Beniwal
Mutations in gyrA are the primary cause of quinolone resistance encountered in gram-negative clinical isolates. The prospect of this work was to analyze the role of gyrA mutations in eliciting high quinolone resistance in uropathogenic E.coli (UPEC) through molecular docking studies. Quinolone susceptibility testing of 18 E.coli strains isolated from UTI patients revealed unusually high resistance level to all the quinolones used; especially norfloxacin and ciprofloxacin. The QRDR of gyrA was amplified and sequenced...
2018: PloS One
https://www.readbyqxmd.com/read/29298125/nontyphoidal-salmonella-enterica-nonsusceptible-to-both-levofloxacin-and-ceftriaxone-in-nebraska-united-states-2014-2015
#15
Caitlin N Murphy, Randal C Fowler, Andrea J Williams, Peter C Iwen, Paul D Fey
Nontyphoidal Salmonella enterica is a common cause of illness in humans ranging from gastroenteritis to invasive disease. National surveillance programs continually monitor trends in antimicrobial resistance patterns and mechanisms of resistance to identify emerging public health threats. Our study shows the emergence of nonsusceptibility to both levofloxacin and ceftriaxone, a concerning phenotype that threatens first-line antibiotic therapy, in Salmonella isolates recovered between 2014 and 2015. From 2010 to 2013 the rate of resistance increased from 0...
January 3, 2018: Foodborne Pathogens and Disease
https://www.readbyqxmd.com/read/29295589/pqsa-promotes-pyoverdine-production-via-biofilm-formation
#16
Donghoon Kang, Kelly E Turner, Natalia V Kirienko
Biofilms create an impermeable barrier against antimicrobial treatment and immune cell access, severely complicating treatment and clearance of nosocomial Pseudomonas aeruginosa infections. We recently reported that biofilm also contributes to pathogen virulence by regulating the production of the siderophore pyoverdine. In this study, we investigated the role of PqsA, a key cell-signaling protein, in this regulatory pathway. We demonstrate that PqsA promotes pyoverdine production in a biofilm-dependent manner...
December 25, 2017: Pathogens
https://www.readbyqxmd.com/read/29290527/mutant-selection-window-of-four-quinolone-antibiotics-against-clinical-isolates-of-streptococcus-pneumoniae-haemophilus-influenzae-and-moraxella-catarrhalis
#17
Hajime Nakai, Takumi Sato, Takashi Uno, Emiko Furukawa, Masato Kawamura, Hiroshi Takahashi, Akira Watanabe, Shigeru Fujimura
Community-acquired pneumonia and otitis media are caused by several bacterial species, including Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. For the treatment of these diseases, various quinolones are frequently used. We determined the mutant prevention concentration (MPC) of four quinolones, levofloxacin, sitafloxacin, tosufloxacin, and garenoxacin, using 92 clinical isolates and evaluated each mutant selection window (MSW). Furthermore, the DNA sequence of the quinolone resistance-determining region (QRDR) for the resistant mutant selected based on the MSW was determined...
December 29, 2017: Journal of Infection and Chemotherapy: Official Journal of the Japan Society of Chemotherapy
https://www.readbyqxmd.com/read/29290430/baicalin-inhibits-escherichia-coli-isolates-in-bovine-mastitic-milk-and-reduces-antimicrobial-resistance
#18
Q Y Zhao, F W Yuan, T Liang, X C Liang, Y R Luo, M Jiang, S Z Qing, W M Zhang
In this study, we aimed to evaluate the inhibitory effect of baicalin on Escherichia coli in vitro and the effects of baicalin treatment on antimicrobial resistance of the E. coli isolates. Through isolation, purification, and identification, a total of 56 E. coli strains were isolated from 341 mastitic milk samples. The study of inhibition effect of baicalin on the E. coli strains in vitro was focused on permeability and morphology of the isolates using an alkaline phosphatase kit and scanning electron microscopy...
December 28, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/29290237/antibiotic-pharmacokinetic-and-pharmacodynamic-parameters-in-pediatric-clinical-practice
#19
R Cohen, E Grimprel
Progress in the knowledge of antibiotic mechanisms of action allows to determine the pharmacodynamics/pharmacokinetic (PK/PD) parameters predictive of antibiotic efficacy in bacterial infections. According to the antibiotic compound, the bacterial species implicated, the location of the infection, and the severity of the disease, these parameters may vary. The PK/PD parameters described in this paper, focus only on blood compartments. These PK/PD parameters best predict efficacy in the most frequent infections (e...
December 2017: Archives de Pédiatrie: Organe Officiel de la Sociéte Française de Pédiatrie
https://www.readbyqxmd.com/read/29287347/quinolones-and-tetracyclines-in-aquaculture-fish-by-a-simple-and-rapid-lc-ms-ms-method
#20
Letícia Rocha Guidi, Flávio Alves Santos, Ana Cláudia S R Ribeiro, Christian Fernandes, Luiza H M Silva, Maria Beatriz A Gloria
The determination of antimicrobials in aquaculture fish is important to ensure food safety. Therefore, simple and fast multiresidue methods are needed. A liquid chromatography tandem mass spectrometry method was developed and validated for the quantification of 14 antimicrobials (quinolones and tetracyclines) in fish. Antimicrobials were extracted with trichloroacetic acid and chromatographic separation was achieved with a C18 column and gradient elution (water and acetonitrile). The method was validated (Decision 2002/657/EC) and it was fit for the purpose...
April 15, 2018: Food Chemistry
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