• 제목/요약/키워드: 1,2,4-Triazole

검색결과 115건 처리시간 0.021초

New Polytriazoleimides with High Thermal and Chemical Stabilities

  • E, Yanpeng;Wan, Liqiang;Li, Yujing;Huang, Farong;Du, Lei
    • Bulletin of the Korean Chemical Society
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    • 제33권7호
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    • pp.2193-2199
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    • 2012
  • A series of novel polytriazoleimides were prepared from various aromatic dianhydrides and a new kind of 1,2,3-triazole-containing aromatic diamine synthesized by the Cu (I)-catalyzed 1,3-dipolar cycloaddition reaction in DMAc, and characterized by FT-IR, $^1H$-NMR, XRD, DSC and TGA techniques. The results show the polytriazoleimides are soluble in most of strong polar solvents and have inherent viscosity values of 0.51-0.62 dL/g(DMAc). The polytriazoleimide films exhibit a tensile strength of 62.3-104.5 MPa and an elongation at breakage of 4.0-8.1%, a glass transition temperature ($T_g$) of $257-275^{\circ}C$, a decomposition temperature (at 5% weight loss) of $350-401^{\circ}C$ in $N_2$ atmosphere, and a dielectric constant of 2.47-3.01 at 10 MHz, which depend on the structure of the polymers. The polytriazoleimides perform good resistance to acid and alkali solution.

단세포전기영동법(single Cell Gel Electrophoresis Assay)을 이용한 농약 살포자의 DNA손상 평가 (Evaluation of DNA damage in Pesticide Sprayers using Single Cell Gel Electrophoresis)

  • 이연경;이도영;이은일;이동배;류재천;김해준;설동근
    • 한국환경성돌연변이발암원학회지
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    • 제21권2호
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    • pp.128-134
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    • 2001
  • Single cell gel electrophoresis (SCGE) assay, also called comet assay, is a rapid and sensitive method to detect DNA damage in single cell level. To evaluate the DNA damage of lymphocytes of pesticides sprayers, SCGE assay was carried out for 50 pesticides sprayer and 58 control subjects. They were interviewed with structured questionnaire to get the information about the kinds and amount of pesticide. Insecticides and fungicides were predominant among pesticides. Major components of pesticides were organophosphorus, organosulfate, cartap, carbamates, and triazole. Sprayed pesticides were classified into two groups. Group I included organophosphorus, organoarsenic, organotin, tetrazine, triazole and gramoxone, which were known to cause DNA damages. Group II pesticide were carbamates, surfactants, organosulfates, etc., which were not found as DNA damaging agents in scientific documents. Olive tail moments of 100 lymphocytes were measured by KOMET 3.1 program for each person. The means of tail moments were compared between farmers exposed to pesticides and control subjects. Farmers showed higher tail moments than control subjects (2.07$\pm$1.40 vs 1.53$\pm$0.77, p<0.05). The means of tail moments also were compared among group I sprayers (n=36), group II sprayers (n=24) and, control subject, and the means or tail moments were 3.4s$\pm$3.2o, 2.66$\pm$2.20 and 1.53$\pm$0.77 respectively. The difference between means of group I sprayers and controls was statistically significant (p<0.05). In conclusion, this study showed higher DNA damage in farmers exposed to pesticides than control subjects, and comet assay could be useful as a biological monitoring method of genotoxic pesticides for farmers.

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Synthesis of New Heterocycles Derived from 3-(3-Methyl-1H-indol-2-yl)-3-oxopropanenitrile as Potent Antifungal Agents

  • Gomha, Sobhi M.;Abdel-Aziz, Hatem A.
    • Bulletin of the Korean Chemical Society
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    • 제33권9호
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    • pp.2985-2990
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    • 2012
  • New thiazoline derivatives 7a-c, and thiophenes 9a-c linked to indole moiety were easily prepared via the reaction of the acrylamide derivative 3 with phenacyl bromides 4a-c, depending on the reaction conditions. In addition, the reaction of compound 3 with hydrazonoyl chlorides 11a-f afforded a series of 1,3,4-thiadiazole derivatives 13a-f. Moreover, coupling of 3-(3-methyl-1H-indol-2-yl)-3-oxopropanenitrile (2) with the diazonium salts of 3-phenyl-5-aminopyrazole 16 or 3-amino-1,2,4-triazole 17 gave the corresponding hydrazones 18 and 19, respectively. Cyclization of the latter hydrazones yielded the corresponding pyrazolo[5,1-c]-1,2,4-triazine and 1,2,4-triazolo[5,1-c]-1,2,4-triazine derivatives 20 and 21, respectively. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, $^1H$ NMR and mass spectral data. All the synthesized compounds were tested for in vitro activities against certain strains of fungi such as Aspergillus niger, Aspergillus nodulans, Alternaria alternate. Compounds showed marked inhibition of fungal growth nearly equal to the standards.

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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    • 제31권12호
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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.

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

  • Nevade, Sidram A.;Lokapure, Sachin G.;Kalyane, Navanath V.
    • 대한화학회지
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    • 제57권6호
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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.

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

  • 김지환;황정인;전영환;김효영;안지운;김장억
    • Journal of Applied Biological Chemistry
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    • 제55권4호
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    • pp.235-239
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    • 2012
  • 사과에 대한 diniconazole과 metconazole의 반감기와 잔류양상을 조사하였다. Diniconazole과 metconazole의 잔류허용기준은 둘 다 1.0 mg/kg으로서 0일차 기준량과 3회 처리구 모두 잔류 허용기준을 넘지 않았다. 재배기간 중 사과의 잔류농도는 약제살포 후 14일 경과 시 diniconazole은 기준량 및 3회 처리에서 0.01 및 0.02 mg/kg으로서 각각 88.9 및 93.8%의 농약이 분해되었다. Metconazole은 각각 0.04 및 0.11 mg/kg으로서 60.0 및 56.0% 정도의 농약 분해율을 보였다. Diniconazole의 사과중 반감기식은 기중량 처리구에서 y=$0.0811e^{-0.179x}$ ($r^2$=0.9693), 3회 처리구에서 y=$0.1451e^{-0.148x}$ ($r^2$=0.9677)이었으며 생물학적 반감기는 각각 3.9일 및 4.7일 이었다. Metconazole의 반감기식은 y=$0.0857e^{-0.055x}$ ($r^2$=0.9242) 및 y=$0.2304e^{-0.052x}$ ($r^2$=0.9544)이었고 생물학적인 반감기는 각각 12.6일 및 13.3일 이었다. Metconazole 기준량과 3회 처리의 경우 first order kinetic model 보다는 second order kinetic mode이 더 적합하였으며 반감기도 기준량에서 2일, 3회 처리에서 1일 감소되는 것을 알 수 있었다. 따라서 각 농약별로 잔류량과 시간과의 관계에 적합한 model을 찾아 반감기를 산출하는 것이 바람직 할 것으로 생각된다.

Synthesis of Novel D-Glucose-derived Benzyl and Alkyl 1,2,3-Triazoles as Potential Antifungal and Antibacterial Agents

  • Wei, Jin-Jian;Jin, Lei;Wan, Kun;Zhou, Cheng-He
    • Bulletin of the Korean Chemical Society
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    • 제32권1호
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    • pp.229-238
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    • 2011
  • A series of novel glucose derived benzyl and alkyl 1,2,3-triazoles and their hydrochlorides have been synthesized via Cu(I)-catalyzed 1,3-dipolar cycloaddition. All the new compounds were characterized by MS, IR and NMR spectra. The DEPT, APT, $^1H$-$^1H$ and $^1H-^{13}C$ 2D NMR spectra for some compounds were also recorded. These compounds were evaluated for their in vitro antibacterial activities against Staphylococcus aureus ATCC 29213, Bacillus subtilis, Bacillus proteus, Pseudomonas aeruginosa, Escherichia coli ATCC 25922, and antifungal activities against Candida albicans and Aspergillus fumigatus. The bioactive data revealed that (3R,4S,5S,6S)-2-(hydroxymethyl)-6-methoxy-4,5-bis((1-octyl-1H-1,2,3-triazol-4-yl)methoxy)-tetrahydro-2H-pyran-3-ol 8a exhibited excellent antifungal activity against A. fumigatus with an MIC value of 0.055 mM compared to Fluconazole. It also showed broad inhibitory efficacy against tested bacterial strains with MIC values ranging from 0.049 mM to 0.39 mM.

HPLC를 이용한 축산물중 잔류페니실린 및 클로람페니콜의 동시분석법 연구 (A study on simultaneous determination of residual penicillin G and chloramphenicol in livestock products by high performance liquid chromatography)

  • 황래홍;윤은선;김현정;김연주;정형기;한인규;이병동
    • 한국동물위생학회지
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    • 제23권1호
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    • pp.1-8
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    • 2000
  • This study was carried out to simultaneous determination of penicillin G and chloramphenicol in livestock products by HPLC. The results obstained were as follows; 1. Penicillin G and chloramphenicol were analyzed by HPLC on symmetry $C_{18}$ column with acetonitrile-0.1 M phosphate buffer containing 0.0157 M thiosulfate (25 : 75) as mobile phase at UV 325nm and 280nm, respectively. 2. Samples were applied to a SeP-Pak $C_{18}$ cartridge, from which eluted penicillin derivatized with 2 M 1,2,4-triazole containing 0.001 M mercuric chloride. 3. The average recovery rates of penicillin G and chloramphenicol were 81.8% and 80.3%, respectively, and the detection limits were 5 ppb (5$\mu\textrm{g}$/kg: 7.9IU/kg) for penicillin G and chloramphenicol in porcine and bovine muscle.

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아자이드와 알킨의 1,3-쌍극자 고리첨가반응에서 고압이 반응속도에 미치는 영향에 대한 연구 (High Pressure Effects on 1,3-Dipolar Cycloaddition of Azides with Alkynes)

  • 권진주
    • 한국군사과학기술학회지
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    • 제18권6호
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    • pp.736-742
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    • 2015
  • The effect of pressure on 1,3-dipolar cycloaddtion has been studied by means of FT-IR and NMR spectroscopy. Pressure accelerates 1,3-dipolar cycloaddition without solvent or catalyst. This simple and inexpensive method eliminates the need for work-up or purification. The method is expected to be applied to the synthesis of binders for solid rocket propellants.

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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    • 제12권2호
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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.