• Bulletin of the Korean Chemical Society
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• 제17권2호
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• pp.147-152
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• 1996

To see the quantitative relationship between the structures of the C-7 substituted quinolones and their antibacterial activities, theoretical parameters such as the molecular van der Waals volume, surface area and some electrostatic parameters based on the molecular electrostatic potential, which represent lipophilicity, and some quantum mechanical parameters are introduced as descriptors. The sixteen substituted quinolone derivatives and twenty bacteria are used for the study. It is found that the QSARs of C-7 substituted quinolones are obtained for eleven bacteria and our descriptors are more useful for Gram positive organisms than negative ones. It is also shown that molecular surface area (or molecular Waals volume) of the C-7 substituent and net charge of C-7 atom of the quinolones are the descriptors of utmost importance.

• 대한화학회지
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• 제51권1호
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• pp.106-110
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• 2007

• Archives of Pharmacal Research
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• 제29권5호
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• pp.369-374
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• 2006

An efficient method for the synthesis of optically active 2-substituted 2,3-dihydro-4-quinolones has been developed. The key features include the introduction of a chiral side chain and the construction of quinolone skeleton by Mitsunobu alkylation and hydroarylation, respectively.

• Bulletin of the Korean Chemical Society
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• 제11권4호
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• pp.313-317
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• 1990

Geometries for several representative quinolone carboxylate type antibacterials have been calculated by computer graphics/molecular mechanics energy minimization procedures using both MM2 and AMBER force fields. The calculated geometries were found to be in reasonable agreements with the corresponding X-ray crystal structures. It has been pointed out that notwithstanding the weaknesses associated with calculating the resonance and hydrogen bonding contributions, the employed methods are capable of generating credible ring geometries and torsional angle dispositions of N(1)-ethyl and 3-carboxylate substituents of the quinolones.

• 약학회지
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• 제55권1호
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• pp.22-31
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• 2011

This systematic review was conducted to assess the clinical effect of ocular fluoroquinolones used for the treatment of bacterial conjunctivitis. A literature search for randomized controlled clinical trials registered up to January 2010 based on PubMed database, using the following search terms: conjunctivitis and fluoroquinolones (besifloxacin, moxifloxacin, gatifloxacin, levofloxacin, lomefloxacin, ciprofloxacin and ofloxacin) were performed. Pooled data on the clinical resolution and bacterial eradication rates derived from selected 16 studies were reported as the relative risk (RR) and 95% confidence interval (95% CI) compared with placebo. Early clinical resolution and microbiological eradication rates in placebo were 28% and 62% respectively. Fluoroquinolones were significantly effective comparing to placebo: early RR 1.94 (95% CI 1.60~2.34) and late RR 1.30 (1.19~1.43) in clinical resolution rates, and early RR 1.75 (1.58~1.94) and late RR 1.28 (1.18~1.39) in microbiological eradication rates. Besifloxacin, ciprofloaxain and moxifloxacin in clinical resolution, and besifloxacin and levofloxacin in microbiological eradication showed higher RRs than pooled overall fluoroquinolones' RRs. New quinolones had higher antibacterial potencies for all pathogens isolated from bacterial conjunctivitis and resistant isolates than old generation quinolones. In conclusion, ocular 7 fluoroquinolones were all effective than placebo for bacterial conjunctivitis and there were differences between quinolones in early and late clinical resolutions and microbiological eradications, and no differences in safety comparing to placebo.

• 한국어병학회지
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• 제36권2호
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• pp.287-292
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• 2023

This study investigated the genetic determinants of plasmid-mediated antibiotic resistance (PMAR) to quinolones and tetracycline in 106 Aeromonas strains isolated from eel (Anguilla japonica, 70 strains) and ornamental fish (36 strains) in Korea. Quinolones and tetracycline resistance phenotypes were found to be widely distributed throughout the both fish groups. However, the prevalence of qnr and tet genes was higher in ornamental fish strains than in eel strains (42.9% vs. 86.1% for qnr and 51.4% vs. 69.4% for tet). In addition, the profiling of the present genetic determinants revealed the dominance of qnrS, tetA, tetE and tetE+qnrS genes for eel strains but of tetA+qnrS qnrS and tetE+qnrS genes for ornamental fish strains. These results indicate that aquaculture and related industries could be a major threat to public health due to the possible spread of PMAR.

• 한국수산과학회지
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• 제48권2호
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• pp.158-167
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• 2015

A lateral flow immunoassay kit based on antigen-antibody interactions was developed to detect residues of beta-lactams, quinolones, tetracyclines, and sulfonamides in farmed fish. Group-specific antibodies showing cross-reactivity with other antibiotics in the same group were produced in rabbits. The rabbits were immunized eight times to obtain the maximum titers. Antibodies were extracted from the antisera collected from the immunized rabbits and produced group-specific reactions with antibiotics from the four groups. A kit was prepared that optimize conditions for the antigen-antibody reaction, using colloidal gold conjugated antibodies, and was designed to detect the four groups of antibiotics simultaneously. The kit enabled the detection of antibiotics in the four groups at below maximum residue limits (MRLs), which were $200{\mu}g/kg$ for tetracyclines, $100{\mu}g/kg$ for sulfonamides, $50{\mu}g/kg$ for beta-lactams, and $100{\mu}g/kg$ for quinolones. The cross-reactivity of the antibodies ranged from 10-80% for the sulfonamides, 20-100% for tetracyclines, 38-100% for quinolones, and 20-100% for the beta-lactams, confirming that the antibodies were group specific. The test kit was used 30 times to examine spiked antibiotics at the limits of detection (LODs) and all produced positive results, indicating high sensitivity. The LODs for the assay ranged from 4-20 ng/mL for beta-lactams, 25-50 ng/mL for sulfonamides, 20-100 ng/mL for tetracyclines, and 30-80 ng/mL for quinolones, and there were no false negative reactions at above these LODs. In addition, all of the LODs of the developed kit were correlated with high-performance liquid chromatography (HPLC) data. Our lateral flow immunoassay kit can simultaneously detect antibiotic residues from a large number of fish samples rapidly, strengthening the safety of domestic farmed and imported fish.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.26-32
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• 1997

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.48-56
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• 1997

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.217.2-218
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• 2001