• 약학회지
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• 제38권5호
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• pp.520-524
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• 1994

A number of 7-[(3-methylthio or methylthiomethyl)-3-pyrrolinyl] quinolone-3-carboxylic acids were synthesised by condensation of 7-fluoro substituted quinolone-3-carboxylic acid with 3-methylthio-3-pyrroline or 3-methylthiomethyl-3-pyrroline. The in vitro antimicrobial activity of them were tested against twenty species of Gram-positive or Gram-negative microorganisms. It showed remarkable antibacterial activity, particularly against Gram-positive microoganisms. Among those 1-cyclopropyl-6,8-difluoro-7-[(3-methylthiomethyl) -3-pyrrolinyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12a) and 1-cycl opropyl-6-fluoro-8-chlore-7-[(3-methylthiomethyl)-3-pyrrolinly]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12b) showed the most potent in vitro antibacterial activity.

• Journal of Microbiology
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• 제45권6호
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• pp.590-592
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• 2007

We report the isolation of Salmonella enterica serotype Typhimurium phage type DT104 (CCARM 8104) from swine in Korea. The CCARM 8104 isolate was resistant to nalidixic acid and showed reduced susceptibility to quinolones. The CCARM 8104 isolate had a missense mutation, Asp87Asn, in the quinolone resistance-determining region in gyrA and produced PSE-1. The CCARM 8104 isolate carried two different class 1 integrons, and the PSE-1 ${\beta}$-lactamase gene was inserted into a 1,200 bp class 1 integron. The presence of DT104 with pse-1 in an integron located in a plasmid and reduced susceptibility to quinolone in swine pose a significant threat of possible horizontal spread between swine and humans.

• Toxicological Research
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• 제8권1호
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• pp.63-70
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• 1992

The present study was performed to evaluate whether the application of Fenbufen is reasonable for predicting the convulsive liability of the quinolone derivatives and to examine whether pentylenetetrazole (PTZ) can be used as a screening tool for their Central Nervous System (CNS) toxic pontential. The convulsive activity of the quinolones was markedly potentiated by the pretreatment of Fenbufen. In combination with Fenbufen, enoxacin (ENX), norfloxacin (XFLX), and ciprofloxacin (CPFX) provoked convlusions and subsequent death at the intravenous doses of 0.5mg/kg, 10mg/kg, and 40mg/kg, respectively, whereas ofloxacin (OFLX) and pefloxacin (PFLX) did not induce convulsions and death even at a relatively high dose of 100mg/kg iv.

• 대한임상검사과학회지
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• 제39권3호
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• pp.161-166
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• 2007

To develop a rapid and reliable single-tube-based PCR technique for detection simultaneously the quinolone resistance qnrA, qnrB and qnrS genes. After multiple alignment, primers were designed to detect known qnr variants. I was used for A total of 43 extented-spectrum ${\beta}$-lactamases (ESBLs) producing Escherichia coli and Klebsiella pneumoniae isolated from university hospital were tested for screening, as with qnr genes. In optimized conditions, all positive controls confirmed the specificity of the PCR primers. Out of 43 isolates, qnrA genes were detected 19 (44.2%), qnrB genes 5 (11.7%), qnrS genes 15 (34.9%) and 8 (18.6%) isolates were not detected. I report here a fast and reliable technique for rapid screening of qnr positive strains to be used for epidemiological surveys.

• Journal of Microbiology and Biotechnology
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• 제30권8호
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• pp.1180-1183
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• 2020

The prevalence and characterization of plasmid-mediated quinolone resistance (PMQR) determinants in ciprofloxacin-resistant Escherichia coli isolated from a Korean commercial layer farm were studied. A total of 45 ciprofloxacin-resistant E. coli isolates were recovered and all isolates were multidrug-resistant. Eight isolates have the PMQR genes aac(6')-Ib-cr, qnrS1, and qnrB4, and seven isolates exhibited double amino acid exchange at both gyrA and parC, and have high fluoroquinolone minimum inhibitory concentrations. Five transconjugants demonstrated transferability of PMQR and β-lactamase genes and similar antimicrobial resistance. Because PMQR genes in isolates from commercial layer chickens could enter the food supply and directly affect humans, control of ciprofloxacin resistance is needed.

• 대한의생명과학회지
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• 제10권4호
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• pp.507-514
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• 2004

The Pseudomonas aeruginosa isolated from the clinical specimens has a mutation on the QRDR (quinolone resistance determining region). There were obvious mutations in both gyrA and parC gene which are major targets of quinolone. Simultaneous mutations were found two sites or more on these genes in all of ten strains. GyrB or parE gene had only silent mutation without converted amino acids. We confirmed that P. aeruginosa from clinical specimens exhibited decreased sensitivity to fluroquiolone due to changed Thr-83→lle and Asp-87→Asn types on gyrA and altered Ser-87→Leu type on parC. This is the first finding that a new Met-93→Thr type on parC as well as mutations on gyrB or parE genes differed from existing patterns. This study showed more mutations of gyrA rather than parC, suggesting that change of Type Ⅳ topoisomerase is more serious than that of type Ⅱ (DNA gyrase).

• Preventive Nutrition and Food Science
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• 제7권2호
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• pp.119-122
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• 2002

Oryza sativa cv. Mihyangbyo is one of several recently developed varieties of rice; characterized by high levels of aromatic components, which may increase its sensory and nutritional properties. In conjunction with our continuing investigation of bioactive components of improved grain varieties, a quinolone alkaloid was isolated from the n-butanol soluble fraction of the aleurone layer of Oryza sativa cv. Mihyangbyo (Gramineae) through activity-guided fractionation and isolation. The compound exhibited moderate antineoplastic activity in a human leukemia cell line (U937) with an $IC_{50}$/ value of 118.1 ug/mL, based on the MTT(3-[4, 5]dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide) cell proliferation assay. The chemical structure of the functional compound was determined, based on physical and spectroscopic characteristics.

• Bulletin of the Korean Chemical Society
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• 제15권12호
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• pp.1070-1079
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• 1994

Quantitative Structure-Activity Relationship (QSAR) studies are performed for the sets of 40 quinolones and 47 naphthyridines. Net charge, van der Waals volume, polarizability, and dipole moment are empolyed as theoretical descriptors(independent variables) to find the relationship between activity and physicochemical properties such as electrostatic effect, steric effect, and transferability. The results are analyzed by the regression and the factor analysis. It is found that for Gram-negative bacteria, the QSAR of quinolone and naphthyridine are substantially different: to describe the activity, the electrostatic effect is the most important for quinolone, and the steric effect and the transferability for naphthyridine.

• 대한화학회지
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• 제42권1호
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• pp.102-104
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• 1998

• 대한화학회지
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• 제41권4호
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• pp.214-218
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• 1997