• Journal of the Korean Chemical Society
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• v.58 no.4
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• pp.366-376
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• 2014

Synthesis, structural characterization, and biological activity studies of novel pyrido[2,3-d]pyrimidines (10a-h, 11a-h) are described. Cyclization of cynoacetamides (4, 5) with malonitrile (7) and aldehyde (6a-h) via Hantzsch pyridine synthesis afforded cyanopyridones (8a-h, 9a-h), which on cyclization with formic acid under microwave conditions led to the final product. All the reactions are significantly faster and the isolated yields are remarkably higher in microwave conditions compared to the conventionally heated reactions. The compounds were tested in vitro for their antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtillus, Staphylococcus aureus, and Micrococcus luteus and antifungal activity against Trichphyton longifusus, Candida albicans, Microsporum canis, Fusarium solani. Compounds 10b, 10e, 11b and 11e exhibited good antibacterial and antifungal activities compared with standards.

• The Plant Pathology Journal
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• v.26 no.3
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• pp.280-285
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• 2010

In the course of a searching natural antifungal compounds from plant sources, we found that the methanol extract ($3,000\;{\mu}g/ml$) of Malus domestica fruits had potential of control against rice blast (Magnaporthe grisea) and tomato late blight (Phytophthora infestans). Under bioassay-guided purification, we isolated phloretin, a phenolic compound, with in vivo antifungal activity against M. grisea. By 1-day protective application of phloretin ($500\;{\mu}g/ml$), the compound strongly inhibited the disease development of M. grisea and P. infestans on rice and tomato seedlings, respectively. And red pepper anthracnose caused by Colletotrichum coccodes also was moderately suppressed. However, rice sheath blight (Rhizoctonia solani AG1), and barley powdery mildew (Blumeria graminis f. sp. hordei) were hardly controlled. In addition, the compound showed in vitro antifungal activity against some plant pathogenic fungi including Phytophthora capsici, Alternaria panax, Sclerotinia sclerotiorum, R. solani AG4, and M. grisea. This is the first report on the antifungal activity of phloretin against plant pathogenic fungi.

• The Plant Pathology Journal
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• v.33 no.6
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• pp.582-588
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• 2017

The objective of this study was to determine inhibitory activities of four volatile plant essential oils (cinnamon oil, fennel oil, origanum oil and thyme oil) on in vitro growth of Fusarium oxysporum f. sp. fragariae causing Fusarium wilt of strawberry plants. Results showed that these essential oils inhibited in vitro conidial germination and mycelial growth of F. oxysporum f. sp. fragariae in a dose-dependent manner. Cinnamon oil was found to be most effective one in suppressing conidial germination while fennel oil, origanum oil and thyme oil showed moderate inhibition of conidial germination at similar levels. Cinnamon oil, origanum oil and thyme oil showed moderate antifungal activities against mycelial growth at similar levels while fennel oil had relatively lower antifungal activity against mycelial growth. Antifungal effects of these four plant essential oils in different combinations on in vitro fungal growth were also evaluated. These essential oils demonstrated synergistic antifungal activities against conidial germination and mycelial growth of F. oxysporum f. sp. fragariae in vitro. Simultaneous application of origanum oil and thyme oil enhanced their antimicrobial activities against conidial germination and fungal mycelial growth. These results underpin that volatile plant essential oils could be used in eco-friendly integrated disease management of Fusarium wilt in strawberry fields.

• 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.

• Bulletin of the Korean Chemical Society
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• v.31 no.12
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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.

• Journal of Veterinary Clinics
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• v.22 no.4
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• pp.371-376
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• 2005

The aim of this study was to determine tile inhibitory effect of granitic powder against Microsporum canis. Fourteen strains of M. canis isolated from dgs and cats with fungal dermatitis and two strains isolated from humans were used in this study. The in vitro antifungal activities of granitic powder and 5 commercialized antifungal agents (terbinafine, itraconazole, ketoconazole, griseofulvin and fluconazole) were compared. The antifungal effect was measured by the broth microdilution method and was expressed as the minimal inhibitory concentration (MIC). The MIC value of the granitic powder was ranged from 31.3 to 250mg/ml. Terbinafine showed the lowest MIC value among the 5 commercial antifungal agents $(0.0078-0.125{\mu}g/ml)$, while fluconazole showed the highest MIC values $(125-1,000{\mu}g/ml)$. The MIC range of itraconazole, griseofuvin and ketoconazole were $0.125-0.5{\mu}g/ml\;0.625-5{\mu}g/ml$ and $10-40{\mu}g/ml$ respectively. The Geometric mean(GM) MIC values of terbinafine and ketoconazole against M. canis isolated from human were $0.0078{\mu}g/ml\;and\;10{\mu}g/ml$, respectively, while the GM MIC values of these agents against M. canis isolated from animals were $0.063{\mu}g/ml\;and\;31.4{\mu}g/ml$, respectively. Other antifungal agents did not show any significant differences in antifungal activity against M. canis of animal or human origin. Although granitic powder was shown to have antifungal activity, it was much lower than that of the 5 commercialized antifungal agents.

• Mycobiology
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• v.35 no.2
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• pp.65-68
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• 2007

Three novel complexes of Cu(II), Co(II) and Zn(II) using a macrocyclic ligand derived by the condensation of diethylphthalate and benzidine have been designed, synthesized and characterized by UV-Vis., IR, Mass and Elemental analyses data in order to find out their antifungal activities. The stoichiometry of the complexes has been found to be 1:1 (Metal: Ligand). The analytical data indicate that the complexes exhibit square-planar geometry. The antifungal activity of the macrocyclic ligand and its metal complexes has been screened in vitro against fungi such as Aspergillus niger, A. flavus, Trichoderma harizanum, T. viridae and Rhizoctonia solani.

• Journal of the Korean Chemical Society
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• v.53 no.6
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• pp.731-741
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• 2009

‘One-pot’ reaction procedure for the synthesis of novel morpholino pyrimidines (10-18) under microwave irradiation in ‘dry media’ in the presence of heterogeneous $NaHSO_4.SiO_2$ catalyst was developed. All the synthesized compounds were screened for their in vitro antibacterial activities against clinically isolated bacterial strains namely Bacillus subtilis, Bacillus cerues, Micrococcus luteus and Salmonella typhii and antifungal activities against fungal strains namely Aspergillus niger, Candida 6 and Candida 51. Structure activity relationship of the synthesized compounds against microbiological results was discussed.

• The Plant Pathology Journal
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• v.18 no.2
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• pp.102-105
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• 2002

A strain of Acremonium strictum, the mycoparasite of Botrytis cinerea, showed strong antifungal activities both in vitro and in vivo against several phytopathogenic fungi. An antifungal substance was purified from the liquid cultures of A. strictum and identified as verlamelin by instrumental analyses. Verlamelin exhibited in vitro antifungal activity against some phytopathogenic fungi such as Magnaporthe grisea, Bipolaris maydis, and Botrytis cinerea, while it was net active against all the bacteria tested. In viva, verlamelin exhibited strong protective and curative activities, particularly against barley powdery mildew. At 100 μg/ml, it inhibited the development of barley powdery mildew with control values of more than 90% in 7-day protective and 2-day curative applications. This is the first report on the production of verlamelin by Acremonium species.

• Bulletin of the Korean Chemical Society
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• v.31 no.5
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• pp.1270-1274
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• 2010

Malassezia is a pathogenic fungus that causes skin diseases, such as tinea versicolor, atopic dermatitis and fatal sepsis. We report the synthesis of a series of benzoxazole amides and evaluation of their antifungal activity against Malassezia furfur. Twelve benzoxazole amides were prepared through the cyclization of the substituted 2-hydroxy aniline with N-(bis-methylsulfanylmethylene) amides. Among the prepared compounds, the compounds 4a, 8b, 8c and 8d showed in vitro antifungal activity.