• Title/Summary/Keyword: 4-Triazole

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Application of Systemic Fungicide for Control of White Muscardine in Silkworm Bombyx mori L.

  • Virendrakumar, B.Nataraju;Thiagarajan, V.;Datta, R.K.
    • International Journal of Industrial Entomology and Biomaterials
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    • v.5 no.2
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    • pp.171-174
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    • 2002
  • Two systemic fungicides, SF1 (Bavistin, a carbandazim fungicide 50% WP, Rallis India ltd., India) and SF2 (Bayleton 25% WP-Triadiamefon, a Triazole compound, Rallis India Ltd., India) were screened for control of muscardine disease in silkworm, Bombyx mori. One and two percent of SF1 and 0.05 and 0.1 % of SF2 in aqueous solution were found to be effective in in vivo condition for the control of the disease. These fungicides, on feeding through mulberry leaves continuously for two days to 4$^{th}$ and 5$^{th}$ instar silkworm larvae inoculated topically with conidia of Beauveria bassiana (4$\times$10$^{6}$ conidia/ml) resulted in reduction in mortality due to muscardine by over 90% as against 100% mortality in inoculated control. SF1 at 1% reduced the mortality by 90% in 4$^{th}$ instar and 91% in final instar silkworm while at 2%, the reduction was 92% and 96%, respectively. SF2 at 0.05 and 0.1 % concentration reduced the mortality by 82 and 88% during 4$^{th}$ instar and by 88 and 92% during 5$^{th}$ instar, respectively.

Effects of 3-Amino-1,2,4 Triazole and Diethyldithiocarbamate on Paraquat Toxicity in Rats (흰쥐에서 Aminotriazole과 Diethyldithiocarbamate가 Paraquat의 독성에 미치는 영향)

  • 차종희;고광삼
    • Toxicological Research
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    • v.13 no.4
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    • pp.393-400
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    • 1997
  • The effects of superoxide dismutase(SOD) and catalase on the toxicity of paraquat(PQ) were studied using diethyldithiocarbamate(DDC), 3-amino-1,2,4-triazole(AT) which are inhibitors of Cu, Zn-SOD and catalase in rats. Sprague Dawley rats were divide into 6 groups: control, DDC, PQ, AT, DDC+PQ, and AT+PQ group. The PQ (50 mg/kg body weight(BW); about half dose of $LD_{50}$) was administered with orally, otherwise AT(1.0g/kg BW) and DDC(1.0g/kg BW) were administered by intrperitoneal(iP) injection. The survival rate of rats in PQ+AT group was significantly decreased compared with PQ group while the difference of survival rate between DDC group and DDC+PQ group was not significant. The SOD activity after administration of DDC was decreased in liver, lung and kidney, but catalase activity was not changed. The catalase activity in liver, lung and kidney of AT treated rats was decreased, while SOD activity was not changed in this group. The effects of DDC and AT to the PQ toxicity was also observed in primary cultured rat Skin fibroblasts. The viable cells that was measured with MTT method, was decreased in AT+PQ treated group compared to PQ treated group, but the difference of cell viability between DDC treat group and DDC+PQ treated group was not observed. This result, AT potentlate PQ toxicity while DDC were not affect, suggested that the decreased catalase activity lead to elevation of hydrogen peroxide levels and PQ toxicity may be correlate with the hydrogen peroxide rather than the superoxides.

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Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position

  • Wubulikasimu, Reyila;Yang, Yanbing;Xue, Fei;Luo, Xianjin;Shao, Dongping;Li, Yuhuan;Gao, Rongmei;Ye, Weidong
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2297-2304
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    • 2013
  • A series of novel benzimidazole derivatives bearing a heterocyclic ring as oxadiazole (21-32), thiadiazole (33-34), triazole (35-36) were synthesized and evaluated for their activities against Coxsackie virus B3 and B6 in Vero cells. Compounds 21-26, 31-36 with moieties of 2'-pyridyl, 3'-pyridyl and 4'-pyridyl at the 2-position and oxadiazoles, thiadiazole, or triazole substituent at the 4- or 5-position generally displayed activities against CVB3 and CVB6. Especially compound 24 ($IC_{50}=1.08{\mu}g/mL$, SI = 61.7 against CVB3) was the promising candidate as lead compound for anti-enteroviral drug. It was observed in the incorporation of heterocyclic rings in benzimidazole at the 5-position could enhance their biological activities.

Antimicrobial Assessment of Some Heterocyclic Compounds Utilizing Ethyl 1-Aminotetrazole-5-carboxylate (Ethyl 1-Aminotetrazole-5-carboxylate로부터 유도된 헤테로고리 화합물들의 항균 활성 시험)

  • Taha, Mamdouh A. M.;El-Badry, Susan M.
    • Journal of the Korean Chemical Society
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    • v.54 no.4
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    • pp.414-418
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    • 2010
  • Ethyl 1-aminotetrazole-5-carboxylate (1) reacted with hydrazine hydrate to give the corresponding aminohydrazide 2. Cyclization of 2 by carbon disulfide yielded 1,3,4-oxadiazole-5-thiol structure 3. Reaction of 3 with either chloroacetone or ethyl chloroacetate furnished S-acyl 1,3,4-oxadiazole derivatives 4 and 5, respectively. Also compound 3 reacted with hydrazine hydrate afforded 4-amino-1,2,4-triazole-5-thiol derivative 6. 6-Methyl-1,3,4-triazolo[3,4-b]-1,3,4-thiadiazole structure 7 was synthesized by reaction of aminothiol 6 with glacial acetic acid. Diazotization of 1 with sodium nitrite in presence of hydrochloric acid yielding the diazonium salt which on treating with hippuric acid, oxazolone derivative 8 was obtained. Furthermore, tetrazolo[5,1-f]-1,2,4-triazine 9 was constructed via cyclization of aminoester 1 with formamide. Compound 9 reacted with carbon disulfide to furnish 8-thione derivative 10 which reacting with chloroacetone, ethyl chloroacetate, and hydrazine hydrate, the corresponding chemical structures 11, 12, and 13 were synthesized. 1,2,4-Triazolo[4,3-d]tetrazolo[5,1-f]-1,2,4-triazines 14 and 15 were resulted by treating of compound 13 with triethyl orthoformate, and glacial acetic acid, respectively. The structures of the newly synthesized products were elucidated according to elemental analyses and spectroscopic evidences. Some of the representative members of the prepared compounds were screened for antimicrobial activity.

A Convenient Synthesis of New 3,7-Diphenylthieno[3,2-e]bis[1,2,4] triazolo[4,3-a:4',3'-c]pyrimidine Derivatives by Oxidative Cyclization Using Alumina-supported Calcium Hypochlorite

  • Son, Hoon-Young;Song, Yang-Heon
    • Bulletin of the Korean Chemical Society
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    • v.31 no.8
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    • pp.2242-2246
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    • 2010
  • New 3,7-diphenylthieno[3,2-e]bis[1,2,4]triazolo[4,3-a:4',3'-c]pyrimidine derivatives were easily synthesized at room temperature in good yield by the oxidative cyclization of thienopyrimidinyl hydrazones with alumina-supported calcium hypochlorite ($Ca(OCl)_2/Al_2O_3$).

Some Reactions of 3-Methyl-5-oxo-1-phenyl-Δ2-pyrazoline-4-thiocarbohydrazide

  • Kandeel, Maymona M.;Abbady, Mohamed S.;Youssef, Mohamed Salah K.
    • Bulletin of the Korean Chemical Society
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    • v.23 no.1
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    • pp.41-47
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    • 2002
  • The reactions of 3-methyl-1-phenyl-5-oxo-${\Delta}^2$-pyrazoline-4-thiocarbohydrazide towards phenyl isothiocyanate, sodium nitrite, cyclohexanone, aromatic aldehydes, and carbon disulphide has been studied. The Vilsmeier-Haack reaction has been applied on 4-substituted pyrazolone derivatives.

Study on the Effects of Corrosion Inhibitor According to the Functional Groups for Cu Chemical Mechanical Polishing in Neutral Environment (중성 영역 구리 화학적 기계적 평탄화 공정에서의 작용기에 따른 부식방지제의 영향성 연구)

  • Lee, Sang Won;Kim, Jae Jeong
    • Korean Chemical Engineering Research
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    • v.53 no.4
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    • pp.517-523
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    • 2015
  • As the aluminum (Al) metallization process was replaced with copper (Cu), the damascene process was introduced, which required the planarization step to eliminate over-deposited Cu with Chemical Mechanical Polishing (CMP) process. In this study, the verification of the corrosion inhibitors, one of the Cu CMP slurry components, was conducted to find out the tendency regarding the carboxyl and amino functional group in neutral environment. Through the results of etch rate, removal rate, and chemical ability of corrosion inhibitors based on 1H-1,2,4-triazole as the base-corrosion inhibitor, while the amine functional group presents high Cu etching ability, carboxyl functional group shows lower Cu etching ability than base-corrosion inhibitor which means that it increases passivation effect by making strong passivation layer. It implies that the corrosion inhibitor with amine functional group was proper to apply for 1st Cu CMP slurry owing to the high etch rate and with carboxyl functional group was favorable for the 2nd Cu CMP slurry due to the high Cu removal rate/dissolution rate ratio.

Influence of Quaternization on UCST Properties of Hydroxyl-Derivatized Polymers

  • Lee, Hyung-Il
    • Bulletin of the Korean Chemical Society
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    • v.35 no.10
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    • pp.3001-3004
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    • 2014
  • A series of hydroxyl-derivatized quaternized polymers were successfully synthesized by atom transfer radical polymerization (ATRP) and Cu(I)-catalyzed 1,3-dipolar cycloaddition of azide and alkynes (click chemistry), followed by quaternization reactions. ATRP was employed to synthesize poly(2-hydroxyethyl methacrylate) (PHEMA), followed by introduction of alkyne groups using pentynoic acid, leading to HEMA-Alkyne. 2-Azido-1-ethanol and 3-azido-1-propanol were combined with the HEMA-Alkyne backbone via click reaction, resulting in triazole-ring containing hydroxyl-derivatized polymers. Quaternization reactions with methyl iodide were conducted on the triazole ring of each polymer. Molecular weight, molecular weight distribution, and the degree of quaternization (DQ) were determined by gel permeation chromatography (GPC) and $^1H$ NMR spectroscopy. The average molecular weight ($M_n$) of the resulting polymers ranged from $5.9{\times}10^4$ to $1.05{\times}10^5g/mol$ depending on the molecular architecture. The molecular weight distribution was low ($M_w/M_n$ = 1.26-1.38). The transmission spectra of the 0.1 wt % aqueous solutions of the resulting quaternized polymers at 650 nm were measured as a function of temperature. Results showed that the upper critical solution temperature (UCST) could be finely controlled by the level of DQ.

Synthesis, Structure and Biological Properties of a Novel Copper (II) Supramolecular Compound Based on 1,2,4-Triazoles Derivatives

  • Qiu, Guang-Mei;Wang, Cui-Juan;Zhang, Ya-Jun;Huang, Shuai;Liu, Xiao-Lei;Zhang, Bing-Jun;Zhou, Xian-Li
    • Bulletin of the Korean Chemical Society
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    • v.33 no.8
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    • pp.2603-2608
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    • 2012
  • A novel mononuclear supramolecule of copper(II) has been synthesized with Ippyt ligand (Ippyt=3-(4'-imidazole phenyl)-5-(pyrid-2''-yl)-1,2,4-triazole) (1). Compound 1, namely [$Cu(Ippyt)_2(H_2O)_2$], has been characterized by single-crystal X-ray diffraction, IR spectrum, elemental analysis and thermogravimetric analysis. Structure determination reveals that the elongated-octahedral geometry is formed in the vicinity of the copper (II) atom being coordinated by four nitrogen atoms from two Ippyt ligands occupying the equatorial position and two oxygen atoms from two coordinated water molecules in the axial position, which together form the $N_4O_2$ donor set. Hydrogen bonding interactions between nitrogen and oxygen atoms result in the set up of a supramolecular network architecture. Biological properties including antibacterial activity and superoxide dismutase (SOD) mimetic activity of compound 1 have been investigated by agar diffusion method and the modified Marklund method, respectively. The results indicate that compound 1 exhibits a stronger antibacterial efficiency than the parent ligand and it also has a certain radical-scavenging activity.

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.