• Title/Summary/Keyword: triazole compounds

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Protective Effects of Thiazolo[3,2-b]-1,2,4-Triazoles on Ethanol­Induced Oxidative Stress in Mouse Brain and Liver

  • Aktay Goknur;Tozkoparan Birsen;Ertan Mevlut
    • Archives of Pharmacal Research
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    • v.28 no.4
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    • pp.438-442
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    • 2005
  • A series of 3-[1-(4-(2-methylpropyl) phenyl) ethyl]-1,2,4-triazole-5-thione (I) and its bicyclic condensed derivatives 6-benzylidenethiazolo[3,2-b]-1, 2,4-triazole-5(6H)-ones (IIa-IIf) were investigated for the prevention of ethanol-induced oxidative stress in liver and brain of mice. Administration of ethanol (0.1 mL/mice, p.o.) resulted in a drop of total thiol groups (T-SH) and non-protein thiol groups (NP-SH), and an increase in thiobarbituric acid reactive substances (TBARS) in both liver and brain tissue of mice (p<0.001). Among the compounds investigated (at a dose of 200 mg/kg, p.o.), I and IId ameliorated the peroxidative injury in these tissues effectively. Compounds IIa, IIc and IIe improved the peroxidative tissue injury only in brain. These findings suggest that certain condensed thiazolo-triazole compounds may contribute to the control of ethanol-induced oxidative stress in an organ selective manner.

Synthesis and Antibacterial Activities of New S-glycosides Bearing 1,2,4-Triazole (1,2,4-Triazole기를 가지고 있는 S-glycoside들의 합성 및 항균활성시험)

  • Chao, Shu-Jun;Geng, Ming-Jiang;Wang, Ying-Ling
    • Journal of the Korean Chemical Society
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    • v.54 no.6
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    • pp.731-736
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    • 2010
  • Several new 5-aryl-3-($\beta$-D-glucopyranosylthio)-1,2,4-triazoles have been synthesized. The structures of these new compounds were confirmed by $^1H$ NMR, $^{13}C$ NMR and elemental analyses.The antibacterial activities of the compounds were also evaluated.

New Thiazolo[3,2-b][1,2,4]triazole Derivatives : Useful Compounds for the Preparation of 7-Substituted Cephalosporins

  • Nam, Ghil-Soo;Lee, Jae-Chul;Chi, Dae-Yoon;Kim, Joong-Hyup
    • Bulletin of the Korean Chemical Society
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    • v.11 no.5
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    • pp.383-386
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    • 1990
  • We have synthesized several bicyclic heteroaromatic compounds with bridgehead nitrogen from N-amine salts of heteroaromatic amines. 2-Amino and 2-unsubstituted thiazolo[3,2-b][l,2,4]triazole derivatives 2a-b were prepared by the cyclization reaction from N-amine salts of aminothiazole-5-yl(N-methoxyimino)acetate with cyanogen bromide and formamidine acetic acid salt, respectively. 2-Methylthiazolo[3,2-b][1,2,4]triazole 2c was obtained from N-acetylated N-amine salt of aminothiazole-5-yl(N-methoxyimino)acetate by the cyclization reaction in the presence of polyphosphoric acid (PPA). 2-Substituted and 2-unsubstituted thiazole[3,2-b][1,2,4]triazole derivatives 2a-c were coupled with 7-aminocephalosporanic acid (7-ACA). Coupled cephalosporin derivatives 1a-c did not have good antibacterial activities in vitro.

Synthesis of [1,2,4]-Triazole Derivatives Containing Benzimidazole and Biological Activities (Benzimidazole을 함유한 [1,2,4]-Triazole 유도체의 합성 및 생물학적 활성)

  • Lee, So-Ha;Jeon, Jae-Ho;Lim, Hye-Won;Pae, Ae-Nim
    • Journal of the Korean Applied Science and Technology
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    • v.23 no.4
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    • pp.355-361
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    • 2006
  • [1,2,4]-Triazole derivatives were synthesized by 5 steps. Benzimidazole was refluxed with ethyl chloroacetate to give 1H-benzimidazole-acetic acid ethyl ester (1) over 52% yield. Ester (1) was refluxed with hydrazine hydrate in the presence of ethanol to afford 1H-benzimidazole-1-acetic acid, hydrazide (2). 5-Benzoimidazol-1-ylmethyl-4H-[1,2,4]triazole-3-thiol (4) was made via coupling of compound (2) with methyl isothiocyanate, followed by cyclization of 1H-benzimidazole-1-acetic acid, 2-[(methylamino) thioxomethyl]hydrazide (3) on reflux, and finally the target compounds (6a-6v) were synthesized by general substitution reaction. Compounds (6a-6v) were screened for T-type calcium channel blocker using the fluorescence assay by FDSS6000. All compounds (6a-6v) did not show better activities than control compound, mibefradil.

Synthesis of 6-Triazole Exomethylenepenams Derivatives (6-트리아졸 엑소메칠렌펜남 유도체의 합성)

  • 김연숙;오정석;임채욱;임철부
    • YAKHAK HOEJI
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    • v.48 no.5
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    • pp.303-308
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    • 2004
  • The synthesis of new 6-triazole exomethylenepenams was described. The 6,6-dibromopenam 5 was reacted with $CH_3$MgBr and substituted triazole 4 to afford the 6-bromo penicillanate 6, which was treated with acetic anhydride to give acetoxy compound 7. The deacetobromination of acetoxy compound 7 with zinc and acetic acid gave 6-exomethylene penams 8 and 9, which were oxidized to sulfones 10 and 11 by m-CPBA. The p-methoxybenzyl compounds 6-11 were deprotected by AlCl$_3$ and neutralized to give the sodium salts 12-17.

Syntheses, Structures, and Characterization of Two Novel Copper(II) and Cadmium(II) Compounds Based on Pyridyl Conjugated 1,2,3-Triazole

  • Hong, Jin-Long;Qu, Zhi-Rong;Ma, Hua-Jun;Wang, Gai-Gai;Zhao, Hong
    • Bulletin of the Korean Chemical Society
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    • v.35 no.5
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    • pp.1495-1500
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    • 2014
  • Two new complexes with 5-methyl-1-(pyridine-3-yl)-1H-1,2,3-triazole-4-carboxylic acid (Hmptc) ligand: [$Cd(mptc)_2(H_2O)_4$] (1) and $[Cu(mptc)_4{\cdot}2H_2O]_n$ (2) were prepared and their crystal structures were determined by single crystal X-ray diffraction analyses. In complex 1, the Cd(II) ions coordinates with the pyridyl nitogen atom from the Hmptc ligand, forming a mononuclear Cd(II) compound. Complex 2 exhibits a novel two-dimensional (2D) polymer in which four Hmptc ligands stabilize the Cu(II) atom. And the coordination involves one nitrogen atom of the triazole, one oxygen atom of the carboxylic acid and the pyridyl nitrogen atom. In addition, FT-IR and solid-state fluorescent emission spectroscopy of two compounds have been determined.

Control Efficacy of Fungicides on Cherry Witches' Broom Caused by Taphrina wiesneri (벚나무 빗자루병균(Taphrina wiesneri)에 대한 살균제의 방제효과)

  • Seo, Sang-Tae;Kim, Kyung-Hee;Shin, Chang-Hoon;Lee, Sang-Hyun;Kim, Young-Mal;Park, Jong-Han;Shin, Sang-Chul
    • Research in Plant Disease
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    • v.15 no.1
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    • pp.13-16
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    • 2009
  • In April 2008, cherry (Prunus yedoensis Matsumura) in Jeju exhibited severe disease of branches forming numerous twigs. Five isolates from diseased leaves were identified as Taphrina wiesneri on the basis of biological and genetic characteristics. Twenty one commercial fungicides were tested for control of the disease in vitro. Of the 21 fungicides, triazole compounds (difenoconazole, propiconazole and tebuconazole) showed relatively good antimicrobial activities. Results from the planta bioassays indicated that triazole compounds reduced the witches' broom disease showing control value $25.7{\sim}52.8%$ compared with the nontreated controls.