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

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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.

Catalase Induced by All-Trans Retinoic Acid Is Involved in Antiproliferation of 36B10 Cells (레티노인산에 의한 카타라제의 유도가 36B10세포의 증식억제에 미치는 효과)

  • Park, Woo-Yoon;Yu, Jae-Ran
    • Radiation Oncology Journal
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    • v.28 no.4
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    • pp.211-218
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    • 2010
  • Purpose: All-trans retinoic acid (ATRA) has anti proliferative effects against brain tumor cells. Recently, ATRA has been reported to induce catalase. We investigated whether catalase induction by ATRA is associated with its anti proliferative effects. Materials and Methods: 36B10 cells were exposed to 0~50${\mu}M$ ATRA for 24 or 48 hours and mRNA, protein, and activity of catalase were measured. Reactive oxygen species (ROS) were measured using 2',7'-dichlorofluorescin diacetate. A clonogenic assay was used to confirm the cytotoxic effect. Results: The mRNA, protein, and activity of catalase were found to increase in a concentration- and incubationtime-dependent manner. The increase in catalase activity induced by ATRA was decreased by the addition of 3-amino-1,2,4-triazole (ATZ). ROS was also increased with ATRA and decreased by the addition of ATZ. The decrease in cell survival induced by ATRA was partly rescued by ATZ. Conclusion: Catalase induction by ATRA is involved in ROS overproduction and thus inhibits the proliferation of 36B10 cells.

Effect on the Inhibition of Over-growth of Plug Seedling by Triazole-type Growth Regulator Treatment (Triazole계 생장조절제 처리가 공정육묘의 도장억제에 미치는 영향)

  • Zhang, Cheng-Hao;Chun, Ik-Jo;Park, Yong-Chul;Kim, Il-Seop
    • Journal of Bio-Environment Control
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    • v.12 no.3
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    • pp.139-146
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    • 2003
  • This study was conducted to investigate the effects on the over-growth inhibition of fruit vegetables (tomato, cucumber, and hot pepper) seedling by the treatment of triazole-typechemicals and to select the most effective chemicals for the over-growth inhibition, and to investigate suitabla concentration treatment and times of the newly selected chemical. The triazole-type chemicals inhibited stem height more, the more the concentration is increased in any crops. The diniconazole showed the highest dwarfing ration, and the tebuconazole and hexaconazole are also good for dwarfing ratio. The diniconazole decreased the plant height of cucumber, tomato, and hot pepper as the concentration is increased. In cucumber, thc dwarfing ratio was 30% in the 5 mg${\cdot}L^{-1}$ treatment, and was 60% in thc l00 mg${\cdot}L^{-1}$ treatment. In tomato and hot pepper, the dwarfing ratio was 30% in the 25 mg${\cdot}L^{-1}$ treatment in any times. In diniconazole treatment, the cucumber and tomato should have 5 mg${\cdot}L^{-1}$ at the lst growth stage and the hot pepper should have 5 mg${\cdot}L^{-1}$ at the 2nd growth stage to obtain good seedlings.

Chemical Modification of Poly(vinylacetylene) and Synthesis of Poly(1,2,3-triazole)s

  • Wang, Lian-Jun;Liao, Shan;Wang, Le-Yong
    • Bulletin of the Korean Chemical Society
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    • v.32 no.5
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    • pp.1471-1474
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    • 2011
  • A series of new polymers containing 1,2,3-triazoles were synthesized and their structures and properties were characterized by FT-IR, $^1H$ NMR, TGA, DSC and GPC. The results showed that the polymers modified by alkyl groups had good solubility, thermal stability and reasonable molecular weights. It was also demonstrated that the properties of fluorine-containing polymers were seriously affected by fluorine atoms with hydrophobic and chemical proof properties.

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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    • v.33 no.9
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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.

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

  • 황래홍;윤은선;김현정;김연주;정형기;한인규;이병동
    • Korean Journal of Veterinary Service
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    • v.23 no.1
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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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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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    • v.32 no.1
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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.

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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Facile Synthesis of Fréchet Type Dendritic Benzyl Azides and Dendrimer via Cycloaddition Reaction with Tripodal Core

  • Lee, Jae-Wook;Kim, Byung-Ku;Kim, Jung-Hwan;Shin, Won-Suk;Jin, Sung-Ho
    • Bulletin of the Korean Chemical Society
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    • v.26 no.11
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    • pp.1790-1794
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    • 2005
  • Fréchet-type dendritic benzyl azides were efficiently synthesized using 5-(azidomethyl)-1,3-dihydroxybenzene as an azide focal point functionalized unit by adding a generation to the existing dendron and applied for the construction of dendrimers containing 1,2,3-triazole rings as connectors via click chemistry with a tripodal acetylene core.

Synthesis of Dendrimer Containing Dialkylated-fluorene Unit as a Core Chromophore via Click Chemistry

  • Han, Seung-Choul;Jin, Sung-Ho;Lee, Jae-Wook
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.137-142
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    • 2012
  • The convergent synthetic strategy for the emissive dendrimers having the chromophore at core via the coppercatalyzed 1,3-dipolar cycloaddition reaction between alkyne and azide was described. 2,7-Diazido-9,9-dioctyl-9H-fluorene, designed to serve as the core in dendrimer, was stitched with the alkyne-functionalized Frechettype and PAMAM dendrons by the click chemistry leading to the formation of the corresponding fluorescent dendrimers in high yields. The preliminary photoluminescence studies indicated that 2,7-diazido-9,9-dioctyl-9H-fluorene showed no fluorescence due to the quenching effect from the electron-rich ${\alpha}$-nitrogen of the azido group but the dendrimers fluoresced due to the elimination of the quenching through the formation of the triazole ring.