• 약학회지
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• 제36권2호
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• pp.110-114
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• 1992

In order to evaluate the antimicrobial effect of 2, 3-substituted-1, 4-naphthoquinone derivatives, we newly synthesized several 2-chloro, 2-bromo and 2-hydroxy-1, 4-naphthoquinones and subjected to antibacterial and antifungal activities, in vitro, against Escherichia coli NIHJ, Staphylococcus aureus ATCC6538p, Candida albicans 10231, Aspergillus niger 1231 and Tricophyton mentagrophytes 6085. Among these derivatives 3, 9, 18 and 23 showed the potent antibacterial activities. 18, 23 and 28 have the antifungal activities. However, these compounds have no significant hemolytic activity at concentrations higher than that required for showing the antibacterial and antifungal activities.

• 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.

• 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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• 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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• 제31권7호
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• pp.2003-2010
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• 2010

A new class of halobenzyloxy or alkoxy 1,2,4-triazoles and their hydrochlorides were synthesized through cyclization starting from commercially available phenylhydrazine. The structures were characterized by MS, IR and $^1H$ NMR spectra as well as elemental analyses. All the synthesized compounds were screened for their antibacterial activities in vitro against Staphylococcus aureus (ATCC29213), methicillin-resistant Staphylococcus aureus (N315), Bacillus subtilis, Escherichia coli (ATCC25922), Pseudomonas aeruginosa, Shigella dysenteriae, Eberthella typhosa, and antifungal activities against Candida albicans (ATCC76615), Aspergillus fumigatus by broth microdilution assay method. The results of preliminary bioassay indicated that 3-(2,4-difluorobenzyloxy)-1-phenyl-1H-1,2,4-triazole hydrochloride exhibited the best inhibitory activity with an MIC value of 56.25 ${\mu}M$ against P. aeruginosa superior to Chloramphenicol, and showed comparable activity with Chloramphenicol against E. coli (ATCC25922).

• KCI Concrete Journal
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• 제14권4호
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• pp.171-177
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• 2002

Antifungal agents are used to impart antibacterial or bactericidal properties to commodities and various articles used in industries and can be classified into two broad groups i.e organic and inorganic. Inorganic antifungal agents comprise of Ag, Zn, or Cu, etc. These elements tend to exhibit high level of antifungal activities, non-uniform dispersion in substrates, and have poor properties in expensive and cheap adhesiveness. In this study, the organic antifungal agent was used for the purpose of investigating the antifungal activity of antifungal agent activated-cement mortar (AACM) on the aspergilus niger of various fungus which can be easily discovered in the interiors and exteriors of buildings. In addition, an experiment on the basic physical properties of AACM such as compressive and flexural strength was carried out. The conclusion of this investigation revealed that a dosage increase of antifungal agent exhibits a high inhibitory effect on the aspergilus niger, and although there is a slight decrease in the strength of AACM, the strength of AACM was almost equal to that of inactivated cement mortar.

• 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.

• Archives of Pharmacal Research
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• 제15권3호
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• pp.263-268
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• 1992

In order to evaluate the antimicrobial effect of 2, 3-disubstitued-1, 4-naphtoquinone derivatives we newly synthesized several 2-bromo-3-(substituted)-1, 4 naphthoquninones. Amination reaction of 2, 3-dihalo-1, 4 naphthoquinones with aryl and aliphatic amines in ethanol gave 2-halo-3-(N-alkyl or N-aryl)1, 4-naphtoquinone derivatives (1a, b-10a, b) i 60% 90%) yield. These derivatives subjected to antibacterial and antifungal activities. in vitro, against Bacilllus subtilis ATCC 6633 Candida albicans 10231 and local, Psudomonas aeruginosa NCTC10490, Staphylococcus aureus ATCC 6538p. Escherichia coli NIHJ Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085. Among these derivatives 1b, 6b and 7a showed the potent antibacterial activities 1b, 8b and 9b have derivatives, 1b, 6b and 7a showed the potent antibacterial activities. 1b, 8b and 9b have the antifungal activities. 1b is most effective in preventing the growth of Bacillus subtilis and Psudomonas aeruginosa. Candida albicans. Aspergillus niger. Tricophyton mentagrophytes. The several of these compounds demonstrated a broad spectrum of activities in vitro.

• 대한화학회지
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• 제53권6호
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• pp.731-741
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• 2009

$NaHSO_4.SiO_2$ 촉매를 이용한 microwave 및 무수조건하에서 새로운 morpholino pyrimidines의 One-pot합성이다. 합성된 모든 화합물을 이용하여 in vitro에서 임상학적인 단리된 박테리아 품종 즉 Bacillus subtilis, Bacillus cerues, Micrococcus luteus , Salmonella typhii에 대해 항균성을 살펴보았고, 균품종 즉 Aspergillus niger, Candida 6, Candida 51에 대해 항진균성을 살펴보았다. 미생물 결과에 대한 합성된 화합물의 구조적 활동성의 관련성에 대해 토론하였다.

• 셀메드
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• 제2권4호
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• pp.37.1-37.4
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• 2012

In the present study, the volatile oil, chloroform extract and methanol extract of the woods of the plants Cedrus deodara and Pinus roxburghii were screened for their antibacterial and antifungal activities against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, Streptococcus pyogenes, Candida albicans, Aspergillus niger, and Aspergillus clavatus using the Agar diffusion method. The susceptibilities of the microorganisms to the extracts were compared with each other and with a selected standard antibiotic. It was observed that the volatile oil and chloroform extracts showed the significant antibacterial activities while the least antibacterial activity was recorded with the methanolic extracts. The higher Minimum Inhibitory Concentration value of the extracts and oils against fungus suggested that the plants may possess less antifungal activity. Phytochemical analysis and thin-layer chromatography profiling revealed the presence of flavonoids and terpenoids in the oil and chloroform extracts, which could explain the antimicrobial activity. The findings suggest that the Cedrus deodara and Pinus roxburghii have antimicrobial properties and they can be used in the treatment of infectious diseases. However, further work is required in order to isolate the active constituents of the plants responsible for the antibacterial activity.