• 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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    • 제21권4호
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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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p-TSA를 이용한 퀴놀론 유도체의 비대칭 이합체 합성 (Synthesis of Asymmetric Dimer of Quinolone Derivatives Using p-TSA)

  • 박명숙
    • 약학회지
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    • 제48권3호
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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.

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 (Synergic Effects of Eunkyo-san and Quinolones on 5 Strains of Aerobic Gram-negative Bacteria)

  • 전귀옥;서영호;권은희;조동희;박미연;최해윤;김종대;송광규
    • 대한한방내과학회지
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    • 제26권3호
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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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인천 유통 수산물 중 잔류동물용의약품 조사 (Monitoring of Residual Veterinary Drugs in Incheon Fishery Products Distribution)

  • 장진섭;허명제;김명희;한영선;권성희;여은영;홍성희;김지선;이승리
    • 한국환경보건학회지
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    • 제44권5호
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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.

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

  • 송동준;서동균;이춘식;배영찬;김원일;김봉환
    • 한국동물위생학회지
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    • 제23권1호
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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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Erythromycin과 tetracycline에 저항성인 Myoplasma pneumoniae의 quinolone계 항생물질에 대한 감수성 (Susceptibilities of Quinolones against Erythromycin- and Tetracycline-Resistant Mycoplasma pneumoniae Isolates)

  • 장명웅;박인달;김광혁
    • 생명과학회지
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    • 제16권5호
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    • pp.799-805
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    • 2006
  • 호흡기 질환 환자로부터 분리된 M. pneumoniae 123 균주를 tetracycline에 저항성인 tetM 유전자만을 가진 36균주, erythromycin에만 저항성 변이를 일으킨 39균주, tetracycline과erythromycin에 저항성인 21균주, erythromycin과 tetracycline에 감수성인 27균주로 나누어 quinolone 제제와 macrolides계 항생제에 대한 감수성 검사를 시험관 희석법으로 실시하여 다음과 같은 결론을 얻었다. Tetracycline에만 저항성인 M. pneumoniae 36균주의 moxifloxacin, levofloxacin, sparfloxacin, ofloxacin, ciprofloxacin, amikacin, clarithromycin에 대한 $MIC_{90}$은 각각 0.125, 0.39, 0.125, 1.0, 1.0, 15.6과 $1.56\;{\mu}g/ml$ 이었다. Erythromycin에만 저항성인 39균주의 $MIC_{90}$은 각각 0.06, 0.39, 0.125, 1.0, 1.0, 15.6과 $25.0\;{\mu}g/ml$ 이었다. Tetracycline과 erythromycin에 모두 저항성인 21 균주의 $MIC_{90}$은 각각 0.125, 0.39, 0.125, 1.0, 1.0, 3.9,과 $1.56\;{\mu}g/ml$ 이었다. Tetracycline과 erythromycin에 모두 감수성인 27 균주의 $MIC_{90}$은 각각 0.125, 0.39, 0.125, 1.0, 1.0, 7.8과 $0.09\;{\mu}g/ml$ 이었다. 이상의 결과로 moxifloxacin, levofloxacin, sparfloxacin 과 같은 quinolone 계 항생물질은 tetracycline이나 erythromycin에 단독 혹은 모두에 저항성인 M. pneumoniae 균주에도 감수성이었으므로 이들 균에 의한 감염증의 치료에 이용할 수 있는 약제이었으나, ofloxacin, ciprofloxacin, clarithromycin 등의 약제 선택에는 항생물질에 대한 감수성검사를 실시하여 적절한 항생제를 선택하는 등의 각별한 주의가 요망된다.