• Journal of the Korean Wood Science and Technology
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• 제40권2호
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• pp.133-140
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• 2012

The antifungal activities of the essential oils from Pinus densiflora, Pinus koraiensis, Abies holophylla, Larix kaempferi, Cryptomeria japonica and Chamaecyparis obtusa against Aspergillus fumigatus were evaluated. Essential oils were extracted from each conifer leaves for 8 h using water distillation method. The essential oil from A. holophylla appeared the strongest antifungal activity among the six oils with MIC value 0.125 mg/$m{\ell}$. The composition of the A. holophylla oil was analysed by GC/MS and then MIC was determined for main constituents of the oil. As the results, borneol and ${\alpha}$-bisabolol, which have a hydroxyl group, showed effective antifungal activities against A. fumigatus (0.25 mg/$m{\ell}$). In addition, the synergistic antifungal effects were observed in the combination of borneol and ${\alpha}$-bisabolol.

• Archives of Pharmacal Research
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• 제17권3호
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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 $1.6\;\mu{g/ml}$.

• Bulletin of the Korean Chemical Society
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• 제31권5호
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• pp.1219-1222
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• 2010

A simple and efficient method has been developed for conversion of arenecarbaldehyde-3-methylquinoxalin-2-ylhydrazones to 3-(2-methylquinoxalin-3-yl)-2-(substitutedphenyl)thiazolidin-4-ones in good yields using microwave irradiation technique on silica as solid support under solvent free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, and mass spectroscopy. All the synthesized thiazolidinones were investigated for their antimicrobial and antifungal activities. The results of the biological activities revealed that the compounds 3b, 3d, 3f and 3h exhibited excellent antibacterial activities while 3d and 3h exhibited good antifungal activity.

• Bulletin of the Korean Chemical Society
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• 제33권8호
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• pp.2627-2634
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• 2012

Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel ${\beta}$-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, $^1H$ nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds (1a-1h) exhibited potent antifungal activities against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 ${\mu}g/mL$. Exhilaratingly, compound 1d (R=3-trifluoromethylphenyl) showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.

• The Plant Pathology Journal
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• 제36권5호
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• pp.491-496
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• 2020

An understanding of the contribution of secondary metabolites (SMs) to the antagonistic and biocontrol activities of bacterial biocontrol agents serves to improve biocontrol potential of the strain. In this study, to evaluate the contribution of each SM produced by Pseudomonas fluorescens NBC275 (Pf275) to its antifungal and biocontrol activity, we combined in silico analysis of the genome with our previous study of transposon (Tn) mutants. Thirteen Tn mutants, which belonged to 6 biosynthetic gene clusters (BGCs) of a total 14 BGCs predicted by the antiSMASH tool were identified by the reduction of antifungal activity. The biocontrol performance of Pf275 was significantly dependent on 2,4-diacetylphloroglucinol and pyoverdine. The clusters that encode for arylpolyene and an unidentified small linear lipopeptide influenced antifungal and biocontrol activities. To our knowledge, our study identified the contribution of SMs, such as a small linear lipopeptide and arylpolyene, to biocontrol efficacy for the first time.

• 생약학회지
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• 제32권2호통권125호
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• pp.140-144
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• 2001

The composition of essential oils in the leaves of three cultivars (Ban-Chung-Gat, Chung-Gat and Dolsan-Gat) of Brassica juncea L. were analyzed and their antifungal activity were investigated in this study. Allyl isothiocyanate, 2-phenyl ethyl isothiocyanate, 4-isothiocyanato-1-butene, 5-methyl isothiazole, benzene acetaldehyde, benzene propane nitrile and beta-ionone have been identified in all of the experimented oils. The main component of the oils from Ban-Chung-Gat and Chung-Gat was 2-phenyl ethyl isothiocyanate while allyl isothiocyanate was the representing compound in the oil of Dolsan-Gat. The antifungal activities of the oils were tested by micro broth dilution method and disc diffusion method. As the result the oils exhibited significant inhibiting activities against Aspergillus niger, A. flavus, Trichoderma viride, Candida albicans, C. utilis, C. tropicalis, Cryptococcus neoformans, Trichosporon mucoides, Trichophyton tonsurans and Geotrichum capitatum.

• Archives of Pharmacal Research
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• 제16권4호
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• pp.327-330
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• 1993

A series of 2-chloro and 2-bromo-3-(substituted)-1, 4-naphthalenedione derivatives (1-25) were tested for antifungal and antibacterial activities in vitro against Candida albicans 10231 aand Local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Fusarium oxysporium KTCC 6501, Bacillus subtilis ATCC 6633, Pseudomonas arruginosa NCTC 10490, Staphylococcus aureus ATCC 6358p, Escherichia coli NIHJ and Acinetobacter baumanii Local. The MiC values were determined by twofold afar diution/streak method. Among thee derivatives, 1, 9, 20, 21, 23 and 25 showed more potent antifungal activities than fluconazole. 20 and 23 completely inhibited the gorwth of fungi, such as Candida albicans, Aspegillus niger, Ticophyton mentagrophytes and fusarium oxysporium, at $3.2\;\mu{g/ml}$. Also some derivatives had the antibacterial activities against Gram-positive bacteria.

• Archives of Pharmacal Research
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• 제25권6호
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• pp.795-800
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• 2002

6,7-Bis-[S-(aryl)thio]-5,8-quinolinediones 4 and 5 were synthesized by the substitution of 6,7-dichloro-5,8-quinolinediones with appropriate arylthiols. Their antifungal activity were tested in vitro for their growth inhibitory activities against pathogenic fungi in comparison with flucytosine. The antifungal activities were significantly improved by S-(aryl)thio moieties of the compounds 4 and 5. The all tested compounds 4 and 5 showed generally good activities against C. albicans and A. niger ranging from 0.8 to 25 $\mu\textrm{g}$/ml. Among them, compounds 4d-4h and 5a-5c exhibited also good activities against C. krusei and C. tropicalis. The activities of compounds 4j and 4I were comparable to those of flucytosine against all tested fungi.

• Bulletin of the Korean Chemical Society
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• 제31권12호
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• pp.3684-3692
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• 2010

A series of azole-containing piperazine derivatives have been designed and synthesized. The obtained compounds were investigated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that most compounds exhibited moderate to significant antibacterial and antifungal activities in vitro. 1-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)-2-(1H-imidazol-1-yl)ethanone and 1-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)-2-(2-phenyl-1H-imidazol-1-yl)ethanone gave remarkable and broad-spectrum antimicrobial efficacy against all tested strains with MIC values ranging from 3.1 to $25\;{\mu}g/mL$, and exhibited comparable activities to the standard drugs chloramphenicol and fluconazole in clinic. Moreover, 2-((4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole was found to be the most effective in vitro against the PC-3 cell line, reaching growth inhibition values (36.4, 60.1 and 76.5%) for each tested concentration: $25\;{\mu}g/mL$, $50\;{\mu}g/mL$ and $100\;{\mu}g/mL$ in dose-dependent manner. The results also showed that the azole ring had noticeable effect on their antimicrobial and cytotoxic activities, and imidazole and benzimidazole moiety were much more favourable to biological activity than 1,2,4-triazole.

• 대한치과보철학회지
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• 제37권3호
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• pp.293-300
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• 1999

The purpose of this study was to evaluate the in vitro antifungal effect of several kinds of denture lining materials containing nystatin and silver-zeolite on Candida albicans. Three commercially available tissue conditioners (Soft-Liner, Coe-Comfort, Coe-Soft) and two direct denture relining materials (Tokuso Rebase, Durabase) were selected. In terms of the zone of inhibition and some basic physical properties, I could find the following results ; 1. Nystatin or silver-zeolite included in those relining materials had definite antifungal activities against the Candida albicans. 2. As times went on, both of the antifungal agents's activities decreased gradually. 3. Antifungal agents did not affect the relining materials' basic physical properties. 4 Direct chairside relining materials showed unfavorable dark discoloration with response to silver-zeolite.