• Title/Summary/Keyword: 1,2,3-Triazole

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Synthesis and Pharmacological Evaluation of Some Novel 2-Mercapto Benzimidazole Derivatives

  • Nevade, Sidram A.;Lokapure, Sachin G.;Kalyane, Navanath V.
    • Journal of the Korean Chemical Society
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    • v.57 no.6
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    • pp.755-760
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    • 2013
  • The present study is synthesis of derivatives of N'-(4-amino-5-sulfanyl-4H-1,2,4-triazole-3-yl)-2-(1H-benzimidazole-2-ylsulfanyl) acetohydrazide (IV). Antibacterial activity tested against the E. coli and A. Substilis. Biological activities conducted by disc diffusion method. Compound $2MB_1$, $2MB_3$, $2MB_5$ inhibit the appreciable microbial growth while rest of the compound possess the moderate activities. Anti-inflammatory activity tested by reduces local edema induced in the rat paw by injection of phlogestic agent. Compound $2MB_1$, $2MB_8$, $2MB_5$, $2MB_3$ and $2MB_6$ exhibit satisfying anti-inflammatory activity while analgesic activity conducted by acetic acid induced writhing effect in mice while compound $2MB_1$, $2MB_4$ and $2MB_7$ having the good analgesic activity. The chemical structures of all newly synthesized compounds were confirmed by their IR, $^1H$ NMR and mass spectral data.

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.

Highly Efficient Phosphorescent White Organic Light-Emitting Devices with a Poly(N-vinylcarbazole) Host Layer

  • Kang, Min-Ki;Moon, Dae-Gyu
    • Transactions on Electrical and Electronic Materials
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    • v.12 no.2
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    • pp.80-83
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    • 2011
  • We have fabricated phosphorescent white organic light-emitting devices (WOLEDs) with a spin-coated poly(Nvinylcarbazole) [PVK] host layer. Iridium(III) bis[(4,6-difluorophenyl)-pyridinato-N,$C^{2'}$]picolinate (FIrpic), tris(2-phenylpyridine)iridium(III) [$Ir(ppy)_3$], and tris(2-phenyl-1-quinoline)iridium(III) [$Ir(phq)_3$], were used as the blue, green, and red guest materials, respectively. The PVK was mixed with FIrpic, $Ir(ppy)_3$, and $Ir(phq)_3$ molecules in a chlorobenzene solution and spin-coated in order to prepare the emission layer; 3-(4-biphenylyl)-4-phenyl-5-(4-tertbutylphenyl)-1,2,4-triazole (TAZ) was used as an electron transport material. The resultant device structure was ITO/PVK:FIrpic:$Ir(ppy)_3:Ir(phq)_3$/TAZ/LiF/Al. The electroluminescence, efficiency, and electrical conduction characteristics of the WOLEDs based on the doped PVK host layer were investigated. The maximum current efficiency of the three wavelength WOLED with the doped PVK host was 19.2 cd/A.

Agricultural Use of the Plant Growth Regulators II. Effect of Uniconazole and Pachlobutrazol Treatment on the Rice Seedling Growth (식물생장조정제의 농업적 이용 연구 II. Uniconazole과 Pachlobutrazol의 토양처리가 벼 묘대기 생육에 미치는 영향)

  • Soon-Chul Kim
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.33 no.3
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    • pp.292-297
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    • 1988
  • kW/1,000 kg in conventionally polished barley and 105 kW/1,000kg in cut-polished barley. Whiteness, water uptake ratio and expanded volume of cooked barley were 45.5, 225.7 and 283% in conventionally polished barley and 49.5, 312.7 and 318% in cut-polished barley, respectively.

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Synthesis of Azole-containing Piperazine Derivatives and Evaluation of their Antibacterial, Antifungal and Cytotoxic Activities

  • Gan, Lin-Ling;Fang, Bo;Zhou, Cheng-He
    • 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.

Patterns of Uptake and Removal by Processing Types of Triazole Fungicides in Onion (Triazole계 살균제의 양파 흡수이행 및 조리 형태별 소실 양상)

  • Lee, Eun-Hyang;Hwang, Jeong-In;Kim, Jang-Eok
    • The Korean Journal of Pesticide Science
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    • v.19 no.3
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    • pp.248-254
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    • 2015
  • Uptake of the triazole fungicides, fluquinconazole and tetraconazole from shoot part of onion was assessed by determining residual amounts of applied fungicides in edible and shoot parts of onion after the foliar application. Combined product of fluquinconazole and tetraconazole (14:7, v/v) as a 21% active ingredient of suspended emulsion formulation was diluted at ratio of 500 and 200 times and sprayed on the shoot part of onion after sealing its root part with absorbent paper. At 10 days after the pesticide application, fluquinconazole residue in the shoot part was the greatest as 5.2 mg/kg at 200 times-dilution treatment, while tetraconazole residue in this part was the smallest as 1.2 mg/kg at 500 times-dilution treatment. On the other hand, the pesticide residues in edible parts of onion at all the treatments were less than limits of detection, 0.01 mg/kg. However, fluquinconazole residues in the edible part of onion divided into three groups such as 1st, 2nd, and 3rd layers were detected at concentrations of 0.04 or 0.24 mg/kg, and these results show the different distribution of pesticides in onion depending on divided layers. In addition, chopped onions were soaked in pesticide solutions prepared with dilution of 1,000 times, cooked using three food processing types such as boiling, stir frying, and pickling, and the pesticide residues in them were analyzed. The analyzed results showed the largest pesticide dissipation in onion followed boiling process (76.9~92.6%).

Determination of Amitrole in Water Samples by Evaporation and GC/MS (증발법과 GC/MS를 이용한 수질 시료 중의 Amitrole의 분석법 연구)

  • Yoon, So Hee;Hong, Ji Eun;Pyo, Hee Soo;Park, Song Ja
    • Analytical Science and Technology
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    • v.16 no.6
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    • pp.483-487
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    • 2003
  • Amitrole is well-known as a non-selective herbicide and it is able to cause contamination of driking water as well as pollution of ground water and surface water. However, it is difficult to extract from water because it has a high solubility for water whereas a low solubility for general organic solvents. This method is described for the determination of amitrole in water samples by GC/MS. After evaporation of 10 mL water sample by a vacuum evaporator, amitrole was derivatized with isobutyl chloroformate (iso-BCF) on room temperature for 15~20 min. As a result, the sensitivity for GCfMS was improved as N-isobutoxycarbonyl amitrole derivative was formed. The linearity of the calibration curve showed good as 0.997. The recoveries were obtained more than 94.9% and relative standard deviations were less than 2.8% at $1.0{\mu}g/L$, $10.0{\mu}g/L$ and $100.0{\mu}g/L$. The limit of detection showed $0.1{\mu}g/L$ with a signal-to-noise ratio (S/N) of 3.

Heterocyclic Systems Containing Bridgehead Nitrogen Atom:Synthesis and Evaluation of Biological Activity of Imidazo[2,1-b]-1,3,4-thiadiazolo [2,3-c]-s-triazoles, s-Triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]quinoxaline and bis-(s-Triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b][imidazo[4,5-b]-cyclohexane]-5a,6a-diene)

  • Kumar, Parvin;Kuamr, Ashwani;Mohan, Late Jag;Makrandi, J.K.
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3304-3308
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    • 2010
  • Condensation of 4-amino-5-mercapto-3-($\alpha$-naphthyl)-s-triazole (1) with cyanogen bromide gives 6-amino-3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazole (2) which on condensation with chloranil yields 3,9-di-($\alpha$-naphthyl)-6,14-dioxo-bis-(s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]cyclohexane]-5a,6a-diene) (3). 3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]quinoxaline (4) is obtained by a similar condensation of (2) with 2,3-dichloroquinoxaline. The reaction of (2) with $\alpha$-haloketones followed by bromination affords 7-aryl-3-($\alpha$-naphthyl)-imidazo[2,1-b]-1,3,4-thiadiazolo[2,3-c]-s-triazoles (5) and their 6-bromo analogues 6 respectively. The structures of all newly synthesized compounds were established on the basis of elemental analyses, IR, $^1H$-NMR. The antibacterial and antifungal activities of all newly synthesized compounds have also been evaluated.

A Density Functional Theory Study of Additives in Electrolytes of a Dye Sensitized Solar Cell

  • Lee, Maeng-Eun;Kang, Moon-Sung;Cho, Kwang-Hwi
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2491-2494
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    • 2013
  • The effect of additives in an electrolyte solution on the conversion efficiency of a dye sensitized solar cell was investigated. A density functional theory (DFT) method was used to examine the physical and chemical properties of nitrogen-containing additives adsorbed on a $TiO_2$ surface. Our results show that additives which cause lower partial charges, higher Fermi level shifts, and greater adsorption energies tend to improve the performance of DSSCs. Steric effects that prevent energy losses due to electron recombination were also found to have a positive effect on the conversion efficiency. In this work, 3-amino-5-methylthio-1H-1,2,4-triazole (AMT) has been suggested as a better additive than the most popular additive, TBP, and verified with experiments.

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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