• Title/Summary/Keyword: Fungicidal

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Three Dimensional Quantitative Structure-Activity Relationship Analyses on the Fungicidal Activities of New Novel 2-Alkoxyphenyl-3-phenylthioisoindoline-1-one Derivatives Using the Comparative Molecular Similarity Indices Analyses (CoMSIA) Methodology Based on the Different Alignment Approaches (상이한 정렬에 따른 비교분자 유사성 지수분석(CoMSIA) 방법을 이용한 새로운 2-Alkoxyphenyl-3-phenylthioisoindoline-1-one 유도체들의 살균활성에 관한 3차원적인 정량적 구조와 활성과의 관계)

  • Sung, Nack-Do;Yoon, Tae-Yong;Song, Jong-Hwan;Jung, Hoon-Sung
    • The Korean Journal of Pesticide Science
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    • v.9 no.1
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    • pp.26-34
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    • 2005
  • 3D-QSAR studies for the fungicidal activities against resistance phytophthora blight (RPC; 95CC7303) and sensitive phytophthora blight (Phytopthora capsici) (SPC; 95CC7105) by a series of new 2-alkoxyphenyl-3-phenylthioisoindoline-1-one derivatives (A & B) were studieded using comparative molecular similarity indices analyses (CoMSIA) methodology. From the based on the results, the two CoMSIA models, R5 and S1: as the best models were derivated. The statistical results of the models showed the best predictability and fitness for the fungicidal activities based on the cross- validated value ($q^2=0.714{\sim}0.823$) and non cross-validated, value ($r^2_{ncv.}=0.918{\sim}0.954$), respectively. The model R5 for fungicidal activity of RPC generated from the field fit alignment and combination of electrostatic field, H-bond acceptor field and LUMO molecular orbital field. The model S1 (or S5) for fungicidal activity of SPC generated from the atom based fit alignment and combination of steric field and HOMO molecular orbital field. The models also shows that inclusion of H-bond acceptor field (A) improved the statistical significance of the models. From the based graphical analyses of CoMSIA contribution maps, it was revealed that the novel selective character for fungicidal activities between the two fungi by modify of X-sub-stituent on the N-phenyl group and R-substituent on the S-phenyl group will be able to achivement.

Efficacy of the Rhinacanthus nasutus Nees Leaf Extract on Dermatophytes with Special Reference to Trichophyton mentagrophytes var. mentagrophytes and Microsporum canis

  • Darah, I.;Jain, K.
    • Natural Product Sciences
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    • v.7 no.4
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    • pp.114-119
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    • 2001
  • The effect of Rhinacanthus nasutus leaf extract on the growth of dermatophytes had been investigated. In vitro the extract exhibited high activity against various species of dermatophytes (Trichophyton mentagrophytes var. mentagrophytes, T. mentagrophytes var. interdigitale, T. rubrum, Microsporum canis and M. gypseum). The minimal inhibitory concentration (MIC) values of the extract revealed that all the dermatophytes tested had MIC values of 13.6 mg/ml. The extract exhibited fungistatic activity at lower concentrations $({\leq}13.6\;mg/ml\;or\;below\;the\;MIC\;value)$ and fungicidal activity at higher concentrations $({\geq}13.6\;mg/ml$\;or\;above\;the\;MIC\;value)$. The results suggested that the extract acted on the cell wall of the dermatophytes which subsequently leading to the formation of cytopathological and membrane structural degeneration and finally leading to cell lysis and death.

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Synthesis, Crystal Structure and Fungicidal Activities of New Type Oxazolidinone-Based Strobilurin Analogues

  • Li, Yuhao;Liu, Rui;Yan, Zhangwei;Zhang, Xiangning;Zhu, Hongjun
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3341-3347
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    • 2010
  • A series of oxazolidinone-based strobilurin analogues were efficiently synthesized by the reaction of 3-(2-bromomethylphenyl) oxazolidin-2-one with 1-substituted phenyl-2H-pyrazolin-3-one. Their structures were confirmed and characterized by $^1H$-NMR, $^{13}C$-NMR, elemental analysis, and mass spectroscopy. In addition, the crystal structure of the target compound 3-(2-((1-phenyl-2H-pyrazol-3-yloxy)methyl)phenyl) oxazolidin-2-one was determined by single crystal X-ray diffraction. The bioassay results of these compounds indicated that some of the oxazolidin-2-one derivatives containing N-substituted phenyl 2H-pyrazol ring exhibited potential in vivo fungicidal activities against M. grisea at the dosage of $1\;g\;L^{-1}$.

In vitro Evaluation of the Antifungal Activity of Propolis Extract on Cryptococcus neoformans and Candida albicans

  • Chee, Hee-Youn
    • Mycobiology
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    • v.30 no.2
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    • pp.93-95
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    • 2002
  • The antifungal activities of propolis on Cryptococcus neoformans and Candida albicans were evaluated. In microbroth culture assay, the MIC(minimum inhibitory concentration) of propolis for C. neoformans and C. albicans were 2 and 16 mg/ml, respectively. In propolis-included solid medium assay, the MIC of propolis for C. neoformans and C. albicans were 4 and 16 mg/ml, respectively. Propolis showed fungicidal activity against C. neoformans, whereas propolis possesed fungistatic activity against C. albicans. The MFC(minimum fungicidal concentration) for C. neoformans was 8 mg/ml. Cell morphology of C. neoformans was affected by treatment of propolis. In scanning electron microscope, the appearance of cell rupture was observed.

Studies on the Synthesis of Naphthoquinoids-1 : Formal Total Synthesis of (+)-6-Oxo-3,4,4a,5-tetra hydro-3-hydroxy-2,2-dimethylnaphtho-1,2-pyran

  • Park, Oee-Sook;Lim, Jae-Gyeong
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.581-585
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    • 1996
  • A new formal total synthesis of (+)-6-oxo-3, 4, 4a, 5-tetrahydro-3-hydroxy-2, 2-dimenthylnaphtho-1, 2-pyran (1) which has been known to have bactericidal, bacteriostatic, fungicidal, fungistatic activities against Staphylococcus aureus and other microorganism, is described. The key reaction involves enantioselective prenylation of .alpha.-tetralone via chiral lithioenamine.

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Inhibition of Fusarium oxysporum f. sp. nicotianae Growth by Phenylpropanoid Pathway Intermediates

  • Shull, Timothy E.;Kurepa, Jasmina;Miller, Robert D.;Martinez-Ochoa, Natalia;Smalle, Jan A.
    • The Plant Pathology Journal
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    • v.36 no.6
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    • pp.637-642
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    • 2020
  • Fusarium wilt in tobacco caused by the fungus Fusarium oxysporum f. sp. nicotianae is a disease-management challenge worldwide, as there are few effective and environmentally benign chemical agents for its control. This challenge results in substantial losses in both the quality and yield of tobacco products. Based on an in vitro analysis of the effects of different phenylpropanoid intermediates, we found that the early intermediates trans-cinnamic acid and para-coumaric acid effectively inhibit the mycelial growth of F. oxysporum f. sp. nicotianae strain FW316F, whereas the downstream intermediates quercetin and caffeic acid exhibit no fungicidal properties. Therefore, our in vitro screen suggests that trans-cinnamic acid and para-coumaric acid are promising chemical agents and natural lead compounds for the suppression of F. oxysporum f. sp. nicotianae growth.

Studies on the Antifungal Action of Leather in Korea (Part. 2) (한국에서의 피혁방미에 관한 연구 2)

  • 김종협;장건형;최춘언
    • Korean Journal of Microbiology
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    • v.3 no.1
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    • pp.18-23
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    • 1965
  • It seems like that the characteristics and drug-resistances of fungi are respectively different in various circumstances. Scores of chemicals were applicated to the leather-fungi in this study. M-dinitrobenzene, 2, 4-dinitrochlorobenzene and phenyl mercuric acetate inhibited the growth of Aspergilli which were isolated from Korean-leather. The minimum fungicidal limits of p-nitrophenol, 8-hydroxyquinoline and sodium-pentachlorophenolate against the Korean-originated strains are different from that of other country. In the mass-screening of fungicides, artificial "Leather-extracts media" have been designed and used, and the media contributed to screening-tests. Fat and oils which are the materials of fat-liquoring in leather manufacture affects the drugresistance of the leather-fungi. It is found that the accelerating-method on malt-agar plate is effective to determinate the fungicidal action of chemicals in short time.hort time.

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Influence of substituted phenoxy group on the fungicidal activities of 2-N-benzyl-5-phenoxy-3-isothiazolone derivatives (2-N-benzyl-5-phenoxy-3-isothiazolone 유도체의 살균활성에 미치는 치환-phenoxy기의 영향)

  • Sung, Nack-Do;Kim, Ki-Hyun
    • The Korean Journal of Pesticide Science
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    • v.5 no.3
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    • pp.36-40
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    • 2001
  • A series of new 2-N-benzyl-5-phenoxy-3-isothiazolone derivatives were synthesized and their in vitro antifungal activities against resistant Phytophthora capsici (RPC) & sensitive Phytophthora capsici (SPC) with metalaxyl fungicide have been measured. In addition, influence of substituted 5-phenoxy group on the -antifungal activities ($pI_{50}$) and the reactivity of substrates were investigated. From the results, reactivity of none substituted substrate showed tendency displaying orbital-controlled reaction. The substituents on the 5-phenoxy ring showed selective fungicidal activity between SPC and RPC. Especially, the 4-fluoro substituent, 6 in the RPC and 4-nitro substituent, 3 in SPC exhibited strongly selective antifungal activity among them. The activities on the SPC would depend largely on the optimal molar refractivity ($MR_{(opt.)}=7.37cm^3/mol$) whereas the activities on the RPC would depend largely on the optimal highest occupied molecular orbital energy ($HOMO_{(opt.)}=-9.2137e.v.$) and weak electron donating (${\sigma}<0$) group. And Free-Wilson analyses revealed that the antifungal activity against RPC depends on the methoxy and bromo-substituent and all of the substituents contribute to antifungal activities against SPC.

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