• Title/Summary/Keyword: 4-Triazole

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Synthesis of 1,2,3-and 1,2,4-Triazole Isonucleosides as Potential antiviral agents

  • Jeong, Soon-Yong;Kim, Myong-Jung;Chun, Moon-Won
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.181.2-181.2
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    • 2003
  • Inosine monophosphate dehydrogenase(IMPDH) catalyzes the $NAD^+$-dependent oxidation of IMP to XMP, the rate limiting step in the de novo biosynthesis of guanine nucleotide. Its critical role at the metabolic branch point in purine nucleotide biosynthesis makes it a useful target in the development of drugs for antiviral and anticancer chemotherapy and in immunosupressant area. Several compound with antiviral activity have been found to be inhibitors of IMPDH. For example, ribavirin, a competitive inhibitor of IMPDH, has broad spectrum antiviral activities against DNA and RNA viruses. (omitted)

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Isolation and Characterization of Soil Bacteria Degrading a Fungicide Defenoconazole (살균제 디페노코나졸 분해 세균 분리 및 특성 분석)

  • Ahn, Jae-Hyung;Ro, Yu-Mi;Lee, Gwan-Hyeong;Park, InCheol;Kim, Wan-Gyu;Han, Byeong-Hak;You, Jaehong
    • The Korean Journal of Pesticide Science
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    • v.20 no.4
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    • pp.349-354
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    • 2016
  • Triazole fungicides occupy an important portion in the global fungicide market and are relatively persistent in soil compared to the other fungicides, suggesting possible adverse effects of the fungicides on human health and environment. In this study, we tried to isolate microorganisms from orchard soils, which can decompose the triazole fungicides, tebuconazole, fluquinconazole, and difenoconazole. Only difenoconazole was completely degraded in the enrichment culture, from which several difenoconazole-degrading bacteria were isolated. They showed the same rep-PCR pattern thus only one strain, C8-2, was further studied. The strain was identified as Sphingomonas sp. C8-2 based on its 16S rRNA gene sequence and decomposed 100 mg/L of difenoconazole in a minimum medium to an unknown metabolite with a molecular weight of 296 within 24 hours. The inhibition effect of the metabolite against representative soil microorganisms significantly decreased compared to that of difenoconazole thus the bacterial strain is expected to be used for the detoxification of difenoconazole in soil and crop.

1,2,4-Triazole Fused Heterocycles; Part 3. Preparation of 1-(1-Phenylethenyl)-5-(N-substituted amino)-1,2,4-triazoles and 4H-1,2,4-Triazolo[1,5-c][1,3,5]oxadiazines

  • 이기정;이유석;송동혁
    • Bulletin of the Korean Chemical Society
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    • v.16 no.11
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    • pp.1037-1042
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    • 1995
  • The reaction of acetophenone 1-ureidoethylidenehydrazones 6 with a mixture of triphenylphosphine, carbon tetrachloride, and triethylamine in dichloromethane provides a general route to 1-(1-phenylethenyl)-5-(N-substituted amino)-1,2,4-triazoles 11 via the electrocyclization of the expected azino carbodiimide intermediates 9 to give the resonance stabilized azomethine imine 10a followed by a proton abstraction from the methyl group by amide anion. However, the same reaction of benzaldehyde 1-ureidoethylidenehydrazones 5 was unsuccessful. Under the same conditions, the reactions of benzaldehyde 1-N-acylureidoethylidenehydrazones 7 or acetophenone 1-N-acylureidoethylidenehydrazones 8 afforded 4H-1,2,4-triazolo[1,5-c][1,3,5]oxadiazines 16 or 17 via the zwitterionic species 15, or a [4+2] intramolecular cycloaddition from the carbodiimide intermediates 14, respectively.

Synthesis of Certain Mercapto and Aminopyrimidine Derivatives as Potential Antimicrobial Agents

  • El-Kerdawy, M.M.;Eisa, H.M.;El-Emam, A.A.;Massoud, M.A.;Nasr, M.N.
    • Archives of Pharmacal Research
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    • v.13 no.2
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    • pp.142-146
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    • 1990
  • Reaction of ethyl 4-chloro-2-phenylpyrimidine-4-carboxylate (4) with 5-chloro-2-methylthiophenol or 3-aryl-4-phenyl-1, 2, 4-triazole-5 thiol yielded the corresponding thioethers (5) and (8a, b), respectively. Careful alkaline hydrolysis of (5) yielded the corresponding carboxylic acid (6). Reaction of (4) with p-aminoacetophenone yielded compound (10) which was reacted with certain aromatic aldehyde to afford the$\alpha,\beta$-unsaturated ketones (11a-d). Condensation of (11a-d) with malononitrile or phenylhydrazine yielded the 2-amino-3-cyanopyridines (12a-f) or the 2-pyrazolines (13a, b) respectively. Seven representative compounds were tested for their in vitro antimicrobial activity against some pathogenic micro-organisms, some of them were proved to be active.

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Electrical and Optical Properties of Phosphorescent Organic Light-Emitting Devices with a TAPC Host

  • Kim, Tae-Yong;Moon, Dae-Gyu
    • Transactions on Electrical and Electronic Materials
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    • v.12 no.2
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    • pp.84-87
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    • 2011
  • We fabricated phosphorescent organic light-emitting devices with a 1,1-bis[(di-4-tolylamino)phenyl]cyclohexane (TAPC) host layer. Two kinds of devices, one of ITO/TAPC/TAPC:FIrpic/TAZ/LiF/Al (device A) and one of ITO/TAPC:FIrpic/TAPC/TAZ/LiF/Al (device B), were prepared to investigate electrical and optical properties. Iridium(III) bis[(4,6-difluorophenyl)-pyridinato-N,$C^{2'}$]picolinate (FIrpic) and 3-(4-biphenylyl)-4-phenyl-5-(4-tert-butylphenyl)-1,2,4-triazole (TAZ) were used as a blue phosphorescent guest material and an electron transport layer, respectively. The TAPC layer in device B strongly contributes to whitish emission, higher driving voltage, and lower current efficiency characteristics compared with device A. The mechanisms of these electrical and optical characteristics of the devices were investigated.

Dissipation Patterns of Triazole Fungicides Estimated from Kinetic Models in Apple (Triazole계 살균제의 사과 중 잔류양상의 Kinetic Model 적용)

  • Kim, Ji-Hwan;Hwang, Jeong-In;Jeon, Young-Hwan;Kim, Hyo-Young;Ahn, Ji-Woon;Kim, Jang-Eok
    • Journal of Applied Biological Chemistry
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    • v.55 no.4
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    • pp.235-239
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    • 2012
  • While cultivating crops, it is important to predict the biological half-lives of applied pesticides to ensure the safety of agricultural products. Dissipation patterns of the triazole fungicides, such as diniconazole and metconazole, during the cultivation of apple were established by utilizing the dissipation curve. As well as, the biological half-lives of the pesticides in apples were calculated using the residue amounts of them. The apples were harvested from 0 to 14 days after spraying diniconazole (WP) and metconazole (SC) at a recommended and three times of the recommended dose. Initial concentrations of diniconazole in apple were 0.09 and 0.15 mg/kg at a recommended and three times of the recommended dose, respectively, which were below MRL 1.0 mg/kg established by KFDA. The equations of biological half-life were $C_t=0.0811e^{-0.179x}$(half life: 3.9 days) and $C_t=0.1451e^{-0.148x}$ (half life: 4.7 days), respectively. In case of metconazole, initial concentrations in apple were 0.10 and 0.25 mg/kg, below MRL 1.0mg/kg, and biological half-life equations were $C_t=0.0857e^{-0.055x}$ (half life: 12.6 days) and $C_t=0.2304e^{-0.052x}$ (half life: 13.3 days), respectively. Therefore, when triazole fungicides were applied during the cultivation of apple, the biological half-life need to be calculated with the optimal equation model.

New Synthesis of Perhydrotriazolotriazoles Catalyzed by TiCl4 under Ambient Conditions

  • Safari, J.;Gandomi-Ravandi, S.;Ghotbinejad, M.
    • Journal of the Korean Chemical Society
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    • v.56 no.1
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    • pp.78-81
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    • 2012
  • Aromatic 2,3-diazabuta-1,3-dienes in glacial acetic acid with isothiocyanate in the presence of catalyst $TiCl_4$ at room temperature produced via criss-cross cycloaddition reactions the corresponding perhydro[1,2,4]triazolo[1,2-a][1,2,4] triazole-1,5-dithiones in relatively high yields and short reaction time.

신규 베타락탐계 항생제 합성과 항균성

  • 고옥현;강형룡;유진철;김경수;홍석순;김영수;황화영;하재천
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.120-120
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    • 1993
  • 목적: Aminothiazole-oxime type의 세파로스 포린계 항생제가 개발되어 제3, 4세대 항생제로 쓰이고 있거나 개발중에 있다. 본 저자들은 pseudomonas균에도 항균력이 우수하고 $\beta$-Iactamase에도 안전하며 기존에 보고된 화합물 보다 개선된 약물을 찾으려는 시도에서 본 연구를 실시하였다. 방법: Cephem의 C-7위치에 aminothiazole methoximetype를 도입시키고C-3위치에 약리 활성이 기대되는 5-(aryl or hot.)-4-phony고-3-mercapto-4H-1,2,4-triazole 화합물들을 합성하여 도입시켜 gram(+), gram(-) 및 fungus균에 대하여 항균력을 실험 하였다. 결과: 합성된 복합물들의 항균력 판정은 Pseudomonas균에는 항균력이 대조 물질 보다 떨어졌으나 몇몇균에 대해서는 대조물질과 비슷한 항균력을 나타내었다.

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Synthesis and Antioxidant Properties of Some Novel Benzimidazole Derivatives on Lipid Peroxidation in the Rat Liver

  • Canan Kus;Gulgun, Ayhan-Kilcigil;Eke, Benay-Can;Mumtaz Iscan
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.156-163
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    • 2004
  • Some benzimidazole derivatives namely 1-[(substituted thiocarbamoylhydrazine carbonyl) methyl]-2-phenyl-1 H-benzimidazoles (1a-13a), N-[(2-phenylbenzimidazol-1-yl methyl)-[1,3,4]-thiadiazole-2-yl]-substituted phenyl amines (1b-13b) and 5-(2-phenyl benzimidazol-1-yl-methyl)-4-substituted phenyl-4H-1,2,4-triazole-3-thiones (1c-13c) were synthesized, and their in vitro effects on the rat liver microsomal NADPH-dependent lipid peroxidation (LP) levels were determined. The most active compound 10a caused an 84% inhibition of LP at $10^{-3}$ M, which is better than that of butylated hydroxytoluene (BHT) (65%).

Effect of Foliar Spray and Soil Drench of Triazole Chemicals on Growth and Flowering in Zinnia elegans (Triazole계 화합물의 엽면살포 및 토양관주 처리가 백일홍의 생장 및 개화에 미치는 영향)

  • Lee, Seung Woo;Ahn, Sung Eun;Kim, Young Chai
    • Horticultural Science & Technology
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    • v.19 no.4
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    • pp.568-573
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    • 2001
  • The effects of foliar spray and soil drench application of triazole chemicals (diniconazole, myclobutanil, difenoconazole, tebuconazole, bitertanol, hexaconazole) on growth and flowering control in zinnia were investigated. For foliar spray application of tebuconazole, diniconazole and bitertanol on 'Dream Land Rose', plant height was decreased but tebuconazole gave the best result for dwarfing. Diameter, fresh and dry weights of flower were markably decreased at high concentration of tebuconazole. However, days to flowering was not affected by chemicals tested. For 'Dream Land Scarlet', plant height was decreased with all chemical treatments. Tebuconazole severely decreased plant height, in particulas. Diniconazole hastened flowering. For soil drench of 'Dream Land Rose', plant height was decreased by diniconazole and mycrobutanil, but diniconazole was more effective for plant height decrease. Flowering was hastened by diniconazole in both 'Dream Land Rose' and 'Dream Land Scarlet'. Plant height of 'Dream Land Scarlet' was decreased by all chemicals tested. Flowering was not occurred at $300mg{\cdot}L^{-1}$ myclobutanil with severe suppression of stem growth.

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