• Title/Summary/Keyword: quinolones

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Synthesis and Biological Activity of 5-hydroxy-4-quinolones and 5-methoxy-4-quinolones as Truncated Acridones

  • Chun, Moon-Woo;Kay Kim Olmstead;Choi, Yong-Seok;Lee, Chong-Ock;Lee, Chong-Kyo;Kim, Joong-Hyup;Lee, Jee-woo
    • Archives of Pharmacal Research
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    • v.21 no.4
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    • pp.445-451
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    • 1998
  • A series of 5-hydroxy-4-quinolone (3) and 5-methoxy-4-quinolone (4) derivatives were synthesized as truncated acridone analogues and evaluated for antitumor, antiheroes and antituberculosis activities. Among them 5-hydroxy-8-methoxy-quinolone showed potent antitumor activity ($IC_{50}$=17.7 $\mu\textrm{M}$ for HL60) which was greater than that of acronycine. However, these compounds didn't show any significant antiheroes or antituberculosis activity.

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Synthesis of Asymmetric Dimer of Quinolone Derivatives Using p-TSA (p-TSA를 이용한 퀴놀론 유도체의 비대칭 이합체 합성)

  • 박명숙
    • YAKHAK HOEJI
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    • v.48 no.3
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    • pp.202-206
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    • 2004
  • New asymmetric dimers, N,N'-dialkyl-4'-hydroxy-4-oxo-2,2',3,3'-tetrahydro-2,2'-diphenyl-4,4'-quinolones 3a-f were synthesized through the dehydration and dea1coholation of N-alkylanilines and ethyl benzoylacetate. Dimers 3a-f were identified by NMR, IR and GC-MS. A series of dimer 3a-f has been synthesized using acid-catalyzed one-pot reaction that involved the condensation, cyc1ization and dimerization. Similarly, the 6,6'-methoxy (or 7,7'-methoxy) substituted dimers were prepared from N-alkyl-meta-(or para)-anisidines. Formation of dimers was undertaken with p-toluenesulfonic acid (p-TSA) at 90∼11$0^{\circ}C$ in toluene for 2∼6 hours over the Dean-Stark apparatus.

Synergic Effects of Eunkyo-san and Quinolones on 5 Strains of Aerobic Gram-negative Bacteria (은교산(銀翹散)과 Quinolone계 항생제의 병용(倂用)이 호기성 Gram(-) 세균주(細菌株)에 대한 시험관내(試驗管內) 항균력(抗菌力)에 미치는 영향)

  • Jeon, Kwi-Ok;Seo, Young-Ho;Kwon, Eun-Hee;Cho, Dong-Hee;Park, Mee-Yeon;Choi, Hae-Yun;Kim, Jong-Dae;Song, Kwang-Kyu
    • The Journal of Internal Korean Medicine
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    • v.26 no.3
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    • pp.521-532
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    • 2005
  • Objectives & Methods : In order to evaluate the in vitro synergic effects or Eunkyo-san which is a traditional poly-herbal formula that has been used in the treatment of respiratory diseases in oriental medicine, and quinolone antibiotics, rufloxacin (RUFX) and iprofloxacin(CPFX), experimentation was designed to determine minimal inhibitory concentration(MIC), $MIC_{50}\;and\;MIC_{90}$ of single use of quinolones and concomitant treatment with Eunkyo-san against 5 strains of aerobic gram negative bacteria, Escherichia coli, Klebsiella peumoniae, Hemophilus influenzae, Citrobacter freundii and Pseudomonas aeruginosae. Result : In the case of aerobic gram negative bacteria, the MIC, $MIC_{50}\;and\;MIC_{90}$ against Klebsiella peumoniae and Citrobacter freundii significantly decreased in concomitant-treated groups with Eunkyo-san compared to those of single-treated groups of RUFX and CPFX, respectively. However, no significant changes were demonstrated against Echerichia coli, Hemophilus influenzae and Pseudomonas aeruginosae. Conclusion : According to these results, concomitant use of Eunkyo-san against some strains of aerobic gram-negative bacteria dramatically increases in vitro antibacterial activity of RUFX and CPFX, and the increase and selectivity of antibacterial activities against these strains is attributable to Eunkyo-san, and not RUFX or CPFX activity.

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Monitoring of Residual Veterinary Drugs in Incheon Fishery Products Distribution (인천 유통 수산물 중 잔류동물용의약품 조사)

  • Jang, Jin-Seob;Hur, Myong-Je;Kim, Meyong-Hee;Han, Young-Sun;Kwon, Sung-Hee;Yeo, Eun-Young;Hong, Seong-Hee;Kim, Ji-Sun;Lee, Seung-Ri
    • Journal of Environmental Health Sciences
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    • v.44 no.5
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    • pp.444-451
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    • 2018
  • Objectives: This study was carried out to provide safe seafood to the public through simultaneous analysis rapid inspections for residual veterinary drugs in 150 fishery products in 2016. Methods: Quinolones (9), Sulfonamides (14), Penicillins (2), Cephalosporins (3), Tetracyclines (4), Macrolides (4), Lincosamides (2), Pleuromutilin (1), Phenicols (4), benzylpyrimidines (2), Others (1) Malachite green (2), and Melamine (1) were analyzed for 49 species using by HPLC and HPLC-MSMS. Results: There were six unsuitable samples, five among fish and one for crustaceans. Within the standard detection were five fish. The antibiotics found were Quinolones (50%), Tetracyclines (33%) and Penicillins (17%). Conclusions: As a result of the experiment, there were six unsuitable samples, five for fish and one for crustaceans. The most prevalent antibiotics were Quinolones. The quinolone antibiotics are highly persistent in fish tissues, so they require more time than the withdrawal period for other common veterinary drugs. Careful attention is required when they are used in fish farms.

Antimicrobial susceptibility features of porcine respiratory bacterial pathogens by modified broth dilution method (돼지 호흡기질병 병인체의 항균제 감수성 조사)

  • 송동준;서동균;이춘식;배영찬;김원일;김봉환
    • Korean Journal of Veterinary Service
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    • v.23 no.1
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    • pp.19-28
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    • 2000
  • There are several main antibacterial susceptibility tests, such as agar dilution method, broth dilution method and disk diffusion technique. Especially, for minimal inhibitory concentration (MIC) test, agar dilution method has been widely used. But that method is so complicated and bothering that it's difficult to treat a large amount of strains. On the other hand, modified broth dilution method(add 1% glucose and 0.018% phenol red as a pH indicator to broth) is fast and easy to perform. Most of all, it can visualize the result by color. The MICs of 22 antibiotics Including penicillins, aminoglycosides, cephalothin, chloramphenicol, lincomycin, ceftiofur, vancomycin and quinolones, erythromycin, colistin. sul-fadimethoxine, trimethoprim for arcanobacterium pyogenes 14 strains, actinobacillus pleuropneu-moniae 41 strains and pasteurella multocida 37 strains, which were collected from porcine during 1996 ∼ 1999, were determined by modified broth dilution method. Actinobacillus pleuropneumoniae was highly susceptible to all kinds of quinolones such as ciprofloxacin, enrofloxacin and norfloxacin and to all aminoglycosides, like gentamicin, apramycin, kanamycin and ampicillin, cephalothin and ceftiofur. But It was quite resistant to solfadimethoxin, colistin and vancomycin. Pasteurella multocida was found to have high susceptibility to ampicillin, cephalothin, chlorampenicol and gentamicin but had mid-degree susceptibility to other aminoglycosides. In addition, it was susceptible to norfloxacin and nalidixic acid, but not to newer fluoroquinolone like ciprofloxacin and enrofloxacin and it was resistant to colistin and kanamycin. Arcanobacterium pyogenes was highly susceptible to most of quinolones such as cipoofloxacin, enrofloxacin and norfloxacin and gentamicin and penicillin G. But it also obtained high resistance against the early quinolone, nalidixic acid and aminoglycosides such as amikacin, apramycin and kanamycin and erythromycin, chlorampenicol, tetracyclin and vancomycin.

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Susceptibilities of Quinolones against Erythromycin- and Tetracycline-Resistant Mycoplasma pneumoniae Isolates (Erythromycin과 tetracycline에 저항성인 Myoplasma pneumoniae의 quinolone계 항생물질에 대한 감수성)

  • Chang, Myung-Woong;Park, In-Dal;Kim, Kwang-Hyuk
    • Journal of Life Science
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    • v.16 no.5
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    • pp.799-805
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    • 2006
  • The in vitro activities of quinolones were determined with 36 strains of tetracycline- resistant, 39 strains of erythromycin-resistant, 21 strains of both resistant to tetracycline and erythromycin, and 27 strains of both susceptible to tetracycline and erythromycin of the M. pneumoniae isolates which have been isolated and classified in previous studies. The $MIC_{90}$ of moxifloxacin, levofloxacin, sparfloxacin, ofloxacin, ciprofloxacin, amikacin, and clarithromycin against 36 strains of tetracycline-resistant M. pneumoniae isolates were 0.125, 0.39, 0.125, 1.0, 1.0, 15.6, and $1.56\;{\mu}g/ml$, respectively. The $MIC_{90}$ against 39 strains of eryhtromycin-resistant M. pneumoniae isolates were 0.06, 0.39, 0.125, 1.0, 1.0, 15.6, and $25.0\;{\mu}g/ml$, respectively. The $MIC_{90}$ against 21 strains of both resistant to tetracycline and eryhtromycin of M. pneumoniae isolates were 0.125, 0.39, 0.125, 1.0, 1.0, 3.9, and $1.56\;{\mu}g/ml$, respectively. The $MIC_{90}$ against 27 strains of both susceptible to tetracycline and eryhtromycin of M. pneumoniae isolates were 0.125, 0.39, 0.125, 1.0, 1.0, 7.8, and $0.09\;{\mu}g/ml$, respectively. These result suggest that moxifloxacin, levofloxacin, and sparfloxacin of the quinolones might be promising antimicrobial agents for the treatment of tetracycline- and erythromycin-resistant M. pneumoniae infection. However, selection of ofloxacin, ciprofloxacin, and clarithromycin for the treatment of M. pneumoniae infection should be cautious decision with antimycoplasmal susceptibility test.