• Archives of Pharmacal Research
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• 제17권6호
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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.

• Journal of Applied Biological Chemistry
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• 제42권3호
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• pp.146-150
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• 1999

As a part of the integrated disease system in greenhouse, an antifungal fungus(AF1) was isolated from greenhouse soil. It exhibited strong inhibitory activites against Pythium ultimum, Phytophtora capsici, Rhizoctonia solani, Botrytis cinerea, and Fusarium oxysporum based on dual culture on 1/5 strength of potato dextrose agar between antagonistic fungus and several plant pathogens. The antagonistic fungus was identified as Chaetomium cochliodes, based on morphological characteristics; the body of the perithecium bears straight or slightly wavy, unbranched hairs, whilst the apex bears a group of spirally coiled hairs. To investigate antagonistic principles, antifungal compound was extracted and fractionated by different solvent systems. An antifungal compound was isolated as pure crystal from is culture filtrate using organic solvent extraction and column chromatography, followed by preparative thin layer chromatography. The chemical structure of the purified antifungal compound was identified as chaetoglobosin A based on the data obtained form $^1H-NMR$, $^{13}C-NMR$, DEPT 90, 135, $^1H-^1H$ COSY, $^1H-^{13}C$ COSY and EI/MS. $ED_{50}$ values of the chaetoglobosin A against P. ultimum, P. capsici, R. solani, B. cinerea and F. oxysporum were 1.98, 4.01, 4.16, 2.67 and 35.14 ppm, respectively.

• 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 $1.6\;\mu{g/ml}$.

• 생약학회지
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• 제25권4호통권99호
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• pp.319-327
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• 1994

A new diterpene, agastanol[1] with dehydroagastol[2] was isolated from th root of Agastache rugosa, and their structures were elucidated by chemical and instrumental analysis. Agastanol[1], its derivatives, agastanone[3] and methylagastanol[5], and dehydroagastol[2] showed cytotoxic activites against in vitro human cancer cell lines. Agastanol[1] showed weak antifungal activity against Trichophyton rubrum.

• Archives of Pharmacal Research
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• 제16권2호
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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.

• Journal of the Korean Wood Science and Technology
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• 제34권3호
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• pp.46-55
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• 2006

본 연구는 피부사상균에 항진균 활성을 보이는 편백정유에 대하여 이를 구성하고 있는 mono- 및 sesquiterpene 성분들 중 어떠한 성분들에 의해 항진균 활성이 나타나는지 탐색하고 성분들 간의 synergy 효과가 존재하는지 알아보고자 피부사상균인 Trichophyton mentagrophytes (KCTC6077), Microsporum canis (KCTC6591), Microsporum gypseum에 대하여 디스크확산법, 한천희석법을 이용하여 항진균 활성을 평가, 비교하였다. Column chromatography를 이용하여 편백정유를 7개(A, B, C, D, E, F, G)로 분획하고, 각각의 분획들에 대하여 한천희석법을 이용하여 T. mentagrophytes에 대한 항진균 활성을 실험한 결과, 분획 D, E, F, G의 항진균 활성이 높았다. GC/MS 분석을 실시하여 높은 항진균 활성을 나타내는 분획의 주성분을 확인하고 그 중 monoterpene인 borneol, linalool, ${\alpha}$-terpineol과, sesquiterpene인 ${\alpha}$-cedrol, nerolidol, ${\beta}$-eudesmol을 선택하였다. 단일 terpene의 항진균 활성 비교 시 monoterpene보다 sesquiterpene이 더 높은 활성을 보였다. 높은 활성을 보이는 sesquiterpene의 단일 및 혼합 성분들과 편백정유의 분획 중 항진균 활성이 높고 sesquiterpene의 함유량이 높은 분획 F의 비교 시, sesquiterpene의 조합 성분들이 높은 항진균 활성을 나타냈다. 이는 sesquiterpene 성분들의 혼합에 의하여 항진균 활성의 synergy 효과가 발현됨을 의미하였다.

• 대한화학회지
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• 제52권1호
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• pp.30-35
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• 2008

연구의 목적은 N1과 6번 자리에 다른 치환기를 가진 5-cyano가 치환된 pyrimidine 아날로그의 새로운 시리즈의 합성과 그것들의 항균성과 항진균성의 활성도에 대해 평가하기 위해서이다. 이 화합물은 MORE technique 를 이용한 potassium carbonate 의 존재하에서 ethylcyanoacetate, 치환된 thioureas, 적당한 알데히드의 제 3차 축합으로 합성 되어졌다. 항균성과 항진균성의 활성도는 25 mg의 농도에서 cup-plate 방법으로 측정되었다. 억제구역은 mm로 측정 되어졌다. 모든 화합물은 좋은 항균성과 항진균성을 보여주었다. P1과 P5는 S.aureus과 E.coli에 대해 최대 활성도를 보여주었고, P6은 모든 종류의 미생물에 대해 좋은 활성도를 보여주었다. P8 화합물은 C. albicans 에 대해 좋은 효과가 있음을 알아냈다. Norfloxacin와 griseofulvin는 합성된 화합물의 활성도와 비교되는 기준물질로 사용되었다. 6번 자리에 p-hydroxy와 p-methoxy로 치환된 phenyl moiety를 가진 gram-양성 미생물에 대해 강력했고, 6번 자리에 이것들이 없는 phenyl moiety 를 가진 아날로그는 gram-음성 활성도를 가졌다,6번 자리에 p-dimethylamino로 치환된 phenyl moiety를 가진 화합물은 적당한 활성을 보여준다.. 게다가 N1자리에서 단지 fluorine을 포함한 아날로그는 상당한 항진균성을 가졌음을 밝혀냈다. N1자리에서 aryl moiety 의 전자 끌게 치환과 마찬가지로 전자 주게 치환은 화합물의 결정된 능력에 중요한 역할을 함을 제시한다.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2003년도 제10차 국제학술회의 및 추계정기 학술발표회
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• pp.48-49
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• 2003

This project was conducted to development several camellia tea mixed herb teas having any physiological effects. Leaves of tea tree contain many compounds, such as polysaccharides, volatile oils, vitamins, minerals, purines, alkaloids(eg. caffeine) and polyphenols(catechins and flavonoids). Although all three tea types(green, oolonr and black) have antibacterial and free radical capturing(antioxidizing) activities, the efficacy decreases substantially the darker the variety of tea is. This is due to lower contents of anti-oxidizing polyphenols remaining in the leaves. Unlike tea tree(Camellia sinensis), the biochemical features and effects of camellia(Camellia japonica) are not well known. Fresh mature leaf of sasanqua camellia(C. sasanqua), roasted young leaf tea(C. japonica) and fresh mature leaf and bark of camellia had high antibacterial activity against P. vulgaris and B. subtilis. In antifungal activity bioassay, young leaf roasted teas of camellia and sasanqua camellia had high activity against C. albicans and T. beigelil. Plant extracts from Camelia japonica had higher inhibitory activity against fungi than against bacteria. In cytotoxic effect against human acute myelogenous leukaemia cell extracts including fresh leaf(200$\mu\textrm{g}$/m1), bark(230$\mu\textrm{g}$/ml) and flower tea (320$\mu\textrm{g}$/m1)inhibited growth of AML cells.(중략)