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Showing 1 to 20 of 21 for “"Quinolones"”.
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The antioxidant properties of 4–quinolones compared to structurally related flavonoids
Oxidative stress is a common occurrence in neuro-degenerative disorders such as Alzheimer's and Parkinson's disease and is suggested to take place before the onset of neuro-degenerative disease, leading to, or exacerbating deterioration. The oxidative status of the cells is regulated by antioxidant …
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Direct arylation of 2-pyrones, coumarins, 2-pyridinones and 2-quinolones
Direct arylation via C-H activation displays a number of advantages over traditional (Suzuki-Miyaura, Stille, etc.) coupling reactions. The 2-pyrone, coumarin, 2-pyridinone and 2-quinolone moieties are prevalent in numerous compounds which exhibit biological activity. In addition, due to the varied …
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Quinolone mechanism of action: sensitivity, mutagenesis and tolerance
… elucidate potential targets for new therapies. Quinolones are an important class of antibiotics that target DNA replication. They bind to topoisomerase II and IV, leading to eventual DNA fragmentation and death. However, the precise mechanism by which they work is not well understood. Because …
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Development of a copper-catalyzed amidation-base-promoted cyclization sequence for the synthesis of 2-aryl- and 2-vinyl1-4 quinolones
… for the preparation of 2-aryl- and 2-vinyl-4-quinolones that utilizes a copper-catalyzed amidation of ortho-halophenones followed by a base-promoted Camps cyclization of the resulting N-(2-keto-aryl)amides is described. With Cul, a diamine ligand, and base as the catalyst system, the amidation …
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Specificity of aldehyde oxidase towards N-heterocyclic cations. Oxidation of quinolinium and related cations by aldehyde oxidase in vitro; the isolation of two products formed simultaneously from a single substrate.
… compounds. The N-heterocyclic cations and quinolones used required synthesis. Incubation of N-methylquinolinium, N-methyl-7,8-benzoquinolinium and N-phenylquinolinium yielded the corresponding 2- and 4-quinolones simultaneously. The ratio of 2- to 4-quinolone formation was found to be …
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The arylation of 2-pyrones and related heterocycles
… such as 2-pyridones, 2-coumarins and 2- quinolones, are useful model substrates to test a novel methodology due to their varied chemical properties. In addition, these moieties possess broad spectrum biological activity. Chapter 1 provides a review of C–H activation methodology as it has …
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Understanding the Genetics and Evolution of Antimicrobial Resistance in Escherichia Coli
… which are known contributors of resistance in quinolones. Resistant isolates had increased resistance levels, widespread cross-resistance to other quinolones, and overall significant costs of resistance in the absence of antibiotic. To investigate novel strategies to combat AMR, I carried out a …
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Strategies to potentiate bactericidal antimicrobial activity based on the suppression of bacterial stress response systems
… SOS response. Certain antimicrobials, such as quinolones and β-lactams, induce the SOS response. Suppression of the SOS response has been shown to enhance the bactericidal activity of antimicrobials such as quinolones. Furthermore, bactericidal antimicrobials such as quinolones are also …
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Synthesis of Aryl Ynol Ethers and Their Synthetic Applications
… reaction to yield hydroxynaphthalenes and quinolones. Moreover, we discovered a hetero-[2+2]-cycloaddition reaction between aryl ketenes and aryl ynol ethers, and the forming cyclobutenones could undergo a retro-4π/6π electrocyclization reaction to afford naphthlenes. Finally, we utilized …
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Geographical Incidence of Antimicrobial Resistant Gonorrhea
… penicillin’s, spectinomycin, tetracycline, quinolones, and other macrolides, have once succeeded at curing gonorrhea. However, once resistance is built, gonorrhea then becomes untreatable. Currently, there are only two medications recommended in the treatment of gonococcal infections: …
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Photocontrol of Antibacterial Activity
… This group was coupled at position 3 of two quinolones antibiotics: nalidixic acid and ciprofloxacin. All photoreleasable quinolones displayed absorption in the visible region varying from the green to the NIR region. Irradiation of the samples with visible light allowed the complete release …
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Anticancer and antibiotic leads from marine organis
… including two phenazines, six 2-alkyl-4-quinolones, and seven rhamnolipids. 2-Nonyl-4(1H)-quinolone and 2-(1-nonenyl)-4(1H)-quinolone displayed potent antimalarial activity, which was first reported here. Based on the metabolic profile of antibiotics from P. aeruginosa, chemical …
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What is the size and nature of the current need for single room isolation in hospital, and how does success or 'failure to isolate' patients affect the control of meticillin-resistant Staphylococcus aureus (MRSA)?
… analysis were: exposure to antibiotics(quinolones and macrolides),presence of a nasogastric tube, dermatological conditions and the index case being risk-assessed as requiring isolation. Further research is needed into the efficacy of isolation in preventing the hospital transmission of …
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Investigations of Carbapenem-resistant Klebsiella species and associated clinical considerations
… Klebsiella spp., have acquired resistance to quinolones, aminoglycosides, cephalosporins and carbapenems. Resistance to β-lactams is mediated via extended-spectrum β-lactamases, AmpC type β-lactamases and carbapenemases combined with porin loss. Carbapenems are the antibiotics of last resort. …
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Secondary ion mass spectrometry imaging of surface-bound microbial communities
… and increase their production of several alkyl quinolones in a dose-dependent manner. Interestingly, the quorum sensing molecule known as Pseudomonas quinolone signal (PQS) was found to be more abundant in regions closest to the antibiotic. These results suggest that PQS is regulated independent …
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The Roles and Regulation of the Redundant Phenazine Biosynthetic Operons in Pseudomonas aeruginosa PA14
… host colonization and (3) phz2 is regulated by quinolones, which are prominent signaling molecules in P. aeruginosa's QS system. We then investigated the roles of individual phenazines in colony development (Chapter 3) and the specificity of SoxR activation by redox active molecules (Chapter 4). …
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Effect of Standard Post-harvest Interventions of Fresh Vegetables on Bacterial Community Dynamics, Pathogen Survival and Antibiotic Resistance
… to the following antibiotic classes: triclosan, quinolones, multidrug, polymyxin and β-lactam (Wilcoxon, p<0.05). No additional increase or reduction of the tet(A) gene present on inoculated P. aeruginosa was evident after 14d storage at 4ºC on irradiated samples. Results of this study suggest …
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Bestimmung des Ausmaßes der Proteinbindung von Arzneistoffen mittels automatisierter kontinuierlicher Ultrafiltration
Das Ausmaß der Proteinbindung eines Arzneistoffs hat Auswirkungen auf eine Vielzahl pharmakokinetischer Parameter wie z.B. das Verteilungsvolumen, die Metabolisierung oder Ausscheidung. Da nur der freie, ungebundene Anteil eines Arzneistoffs durch bio-logische Membranen diffundieren kann, ist …
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Phosphodiesterase 4 inhibitors for the treatment of inflammation associated with respiratory disease
… examined were xanthines, aryl sulphonamides, quinolones, 7-methoxybenzofuran-4-carboxamides, and 7-methoxyfuro[2,3-c]pyridine-4-carboxamides. The lead molecules selected in each publication had improved PDE4:RBA ratios which translated into an improved therapeutic window in vivo. These …
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The Total Synthesis of Pseudonocardia sp. Quinolone Natural Products and Studies Towards the Total Synthesis of 1β-Hydroxyalantolactone
Natural products have long been known for their broad range of useful therapeutic properties, and have been widely utilised in the field of medicine. This dissertation describes work towards the total synthesis of natural products possessing biological activity in two important areas. The first …
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