• Title/Summary/Keyword: antifugal

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The Synthesis of 6-(N-Arylamino)-7-Chloro-5,8-Quinolinedione Derivatives for Evaluation of Antifugal Activities

  • Ryu, Chung-Kyu;Kim, Hee-Jeong
    • Archives of Pharmacal Research
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    • v.17 no.3
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    • pp.139-144
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    • 1994
  • A series of 6-(N-aylamono)-7-chloro-5, 8-quinolinedione derivatives was newly synthesized for the evaluation of antifugal activities. 5-Amino-8-hydroxy-quinoline (II) was treated with $KCLO_3$ in HCl to give 6,7-dichloro-5,8-quinolinediones (III). 6-(N-Arylamino)-7-chloro5,8-quinolinediones 1-13 were prepared by regioselective nucleophilic substitution of III with arylamines. In the presence of $CeCl_3$, the N-arylamono groups were introduced at the 6-position of 5,8-quinolinedione ring by the regioselective substitution. These derivatives 1-12 were tested for natifungal and also antibacterial activites, in vitro, against Canadida albicans, Aspergillus nier, Tricophyton mentagrophytes, Bacillus subtilis, Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coil. The MIC values were determined by the two-fold agar/steak dilution method. Newly obtained 6-(N-arylamino)-7-chloro5,8-quinolinedione derivatives showed potent antifungal and antibacterial activities. Among these derivatives, 1,3,5,7,8 and 9 showed more potent antifungal activities than fluconazole and griseofulvin. Also most of derivatives were found to be more active than ampicillin against gram-positive bacteria. 1 and 7 showed the very potent antifungal activities. 1 was the most efective in preventing the growth of Candida albicans, Aspergillus niger, Tricophyton mentagrophytes, Bacillus subtills and Staphylococcus aureus at MIC $1.6\;\mu{g/ml}$.

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The Antifungal Activities of some 6-[N-(halophenyl)amino]-7-Chloro-5,8-Quinolinediones against Candida Species

  • Ryu, Chung-Kyu;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.17 no.6
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    • pp.483-486
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    • 1994
  • A series of 6-[N-(halophenyl)amino]-7-chloro-5, 8-quinolinedione derivatives 1-10 were tested for antifungal susceptibilities, in vitro, aginst pathogenic Candida species such as C. ablbicans, C glabrata, C. krusei, C. parapsilosis and C. tropicalis. The MICs were determined by the standard macrodilution techniques, according to the NCCLS 1992 guidelines. The 6-[N-(halo-standard macrodilution techniques, according to the NCCLS 1992 gidelines. The 6-[N-(halo-phenyl)amino]-7-chloro-5, 8-quinolinedione derivatives showed generally potent antifungal activities against pathogenic Candida species. Among them, derivative 1, 2, 5, and 7 showed more potent antifungal activities than kietoconazole. All derivatives 1-10 had specially potent activities against C. torpicalis. Derivative 1 and 2 containing 9N-3, 4-dihalo-phenyl)amino moiety exhibited the potent antifugal activities. Derivative 2 with (3, 4-dichlorophenyl)amino substitutent was the most effetive in preventing the growth of Candida species at MICs 4.mu.g/ml respectively.

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The antimicrobial Activities of Some 1,4-Naphthalenediones (III)

  • Ryu, Chung-Kyu;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.161-163
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    • 1993
  • In order to evaluate the antimicrobial effect of 2,3-disubstituted-1,4-naphthalenedione derivatives, we synthesized several 2-chloro, 2-bromo and 2-hydroxy-3(substituted)-1, 4-naphthalene-diones (1-25). These derivatives were tested for antifugal and antibacterial activities, in vitro, against Candida albicans 10231 and local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Baciilus subtilis ACTT 6633, Pseudomonas aeruginsa NCTC 10490, Staphylococcus aureus ATCC 6538P, Escherichia coli NIHJ. The MIC values were determined by the two-fold agar dilution/strea method. Among these derivatives, 4, 5 and 6 showed the potent antifungal activities. Also 5 and 6 had the antibacterial activities. 5 with (1,2,4-triazolyl)-amino moirty was the most effective in preventing the growth of fungi, such as Candida albicans, Aspergillus niger and Tricophyton mentagrophytes.

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Impact of transgenic AFPCHI (Cucumis melo L. Silver Light) fungal resistance melon on soil microbial communities and enzyme activities

  • Bezirganoglu, Ismail;Uysal, Pinar
    • Journal of Plant Biotechnology
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    • v.44 no.2
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    • pp.156-163
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    • 2017
  • A greenhouse experiment was conducted for evaluation of ecological effects of transgenic melon plants in the rhizospheric soil in terms of soil properties, enzyme activities and microbial communities. Organic matter content of soil under transgenic melon plants was significantly higher than that of soil with non-transgenic melon plants. Significant variations were observed in organic matter, total P and K in soil cultivation with transgenic melon plants. There were also significant variations in the total numbers of colony forming units of fungi, actinomycetes and bacteria between soils treated with transgenic and non-transgenic melon plants. Transgenic and non-transgenic melon significantly enhanced several enzymes activities including urease, acid phosphatase, alkalin phosphatase, arysulphtase, ${\beta}$ glucosidase, dehydrogenase, protease and catalase. Soil polyphenoloxidase activity of $T_1$ transgenic melon was lower than that of $T_0$ transgenic melon and a non-melon plant during the same period. The first generation transgenic melon plants ($T_0$) showed significantly greater (p<0.05) effect on the activitiy of arylsulfatase, which increased from $2.540{\times}10^6CFU\;g^{-1}$ (control) to $19.860{\times}10^6CFU\;g^{-1}$ ($T_0$). These results clearly indicated that transgenic melon might change microbial communities, enzyme activities and soil chemical properties.

Production of $\alpha$-Glucosidase Inhibitor by $\beta$-Glucosidase Inhibitor-Producing Bacillus lentimorbus B-6

  • Kim, Kyoung-Ja;Yang, Yong-Joon;Kim, Jongkee
    • Journal of Microbiology and Biotechnology
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    • v.12 no.6
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    • pp.895-900
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    • 2002
  • A soil microorganism producing ${\alpha}$- and ${\beta}$-glucosidase inhibitors was identified as Bacillus lentimorbus, based on the fatty acid and morphological analyses, along with biochemical and physiological tests. The ${\alpha}$-glucosidase inhibitor was highly produced by this strain in a culture medium containing $0.25\%$ of sodium glutamate and $0.5\%$ of glucose, pH 8.0 at $30^{\circ}C$ for 2 days. The ${\alpha}$-glucosidase inhibitor from culture filtrate of his strain was identified as water soluble, organic solvent nonextractable, and heat stable. In addition to ${\alpha}$-glucosidase inhibitor, this strain also produced ${\beta}$-glucosidase inhibitor in he same culture medium and this inhibitor showed an antifugal activity against Botrytis cinerea. While the production of ${\alpha}$- glucosidase inhibitor was decreased by a glucose concentration higher than $1\%$, the production of ${\beta}$-glucosidase inhibitor was lot Influenced by a glucose concentration higher than $20\%$. The ${\alpha}$-glucosidase inhibitor from culture filtrate of this strain was separated from the ${\beta}$-glucosidase inhibitor through Sephadex G-100 column chromatography.

The antifungal activity and growth promotion effects of Bacillus sp. LP03, TBM40-3 on Pohang Buchu (Leeks). (포항 부추에 대한 biosurfactant를 생산하는 Bacillus sp. LP03, TBM40-3의 항진균성과 생육에 미치는 영향)

  • 장혜원;최용락;주우홍;최윤혁;도형기;황철원
    • Journal of Life Science
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    • v.14 no.5
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    • pp.859-862
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    • 2004
  • This report investigates antifungal activity and effects of growth promotion by biosurfactant produced from Bacillus sp. LP03 and TBM40-3 against fungus causing plants disease (Glay Mold-Botrytis cinerea). Antifugal activity against B. cinerea infeeted to leek (Allium tuberosum Rottler) exhibited better than antifungal agent farming drug (smilex, Dong bang agro., Seoul, Korea.) through the field test. After infected by plant's disease, the leaves growth and number are maintained under presenting biosurfactant produced strains. Especially, one of the strains, named Bacillus sp. LP03 showed strong antifungal activity on field studies.

Antifungal Activity of EDTA and Combinatory Synergism of EDTA with Polygodial against Saccharomyces cerevisiae (Saccharomyces cerevisiae에 대한 EDTA의 항진균 활성 및 EDTA와 Polygodial 간의 병용 효과)

  • Lee, Sang-Hwa;Lee, Jae-Ran;Kim, Chang-Jin
    • Korean Journal of Food Science and Technology
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    • v.31 no.4
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    • pp.1109-1114
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    • 1999
  • The antifungal activity of ethylenediaminetetraacetic acid (EDTA), an antioxidative food preservative, was investigated against Saccharomyces cerevisiae. At the general condition for antifugal test, EDTA exhibited the minimum inhibitory concentration (MIC) of 200 ${\mu}g/ml$ and the minimum fungicidal concentration (MFC) of 6,400 ${\mu}g/mL$, As seen with the antibacterial activity, the antifungal activity of EDTA was greatly decreased by high inoculum size, acidic medium, and cation ($Ca^{++},\;or\;Mg^{++}$) added to medium. On the other hand, when EDTA was combined with polygodial isolated from natural food spice, they showed strong synergism on the antifungal activity. Further, the diminishing antifungal activity of EDTA by high inoculum size, acidic medium, and cation ($Ca^{++}\;or\;Mg^{++}$) added to medium was considerably improved by the combination with polygodial.

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Confirmation of Non-Siderophore Antifugal Substance and Cellulase from Bacillus lichemiformis Kll Containing Antagonistic Ability and Plant Growth Promoting Activity (생물방제능과 식물성장촉진능을 동시에 가지는 Bacillus licheniformis K11의 non-siderophore 항진균 물질 및 cellulase의 생산조건 확인)

  • Woo, Sang-Min;Kim, Sang-Dal
    • Journal of Life Science
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    • v.17 no.7 s.87
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    • pp.983-989
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    • 2007
  • Bacillus lichemiformis Kll, a plant growth promoting rhizobacterium was reported as a producer of auxin, siderophore, as well as antifungal cellulase under some culture conditions. In vitro test, B. licheniformis Kll represented excellent antagonistic ability against Fusarium oxyspoum (KACC 40037), and showed broad spectrum against other phytopathogenic fungi. B. licheniformis Kll had cellulolytic activity toward not only carboxymethyl-cellulose (CMC) but also insoluble cellulose, such as fungal cell wall cellulose, filter paper (Whatman No. 1), and Avicel. In addition, we confirmed antifungal substance production by butanol-extract methods. The strain produced optimally the antifungal substance when it was cultivated at pH 9.0, 30${\circ}$C for 4 days on nutrient medium. The biological control mechanisms of B. lichemiformis Kll were caused by antifungal substance, cellulase and siderophore against phytopathogenic fungi.