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

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Mechanism Studies of Substituted Triazol-1-yl-pyrimidine Derivatives Inhibition on Mycobacterium tuberculosis Acetohydroxyacid Synthase

  • Chien, Pham Ngoc;Jung, In-Pil;Reddy, Katta Venugopal;Yoon, Moon-Young
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4074-4078
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    • 2012
  • The first step in the common pathway for the biosynthesis of branched chain amino acids is catalyzed by acetohydroxyacid synthase (AHAS). The AHAS is found in plants, fungi and bacteria. With an aim to identify new anti-tuberculosis drugs that inhibit branched chain amino acid biosynthesis, we screened a chemical library against Mycobacterium tuberculosis AHAS. The screening identified four compounds, AVS 2087, AVS 2093, AVS 2236, and AVS 2387 with $IC_{50}$ values of 0.28, 0.21, 3.88, and $0.25{\mu}M$, respectively. Moreover, these four compounds also showed strong inhibition against reconstituted AHAS with $IC_{50}$ values of 0.37, 0.26, 1.0, and $1.18{\mu}M$, respectively. The basic scaffold of the AVS group consists of 1-pyrimidin-2-yl-1H-[1,2,4]-triazole-3-sulfonamide. The most active compound, AVS 2387, showed the lowest total interaction energy -8.75 Kcal/mol and illustrates its binding mode by hydrogen bonding with $H_{\varepsilon}$ of Gln517 with the distance of $2.24{\AA}$.

Purification and Characterization of Catalase-2 from Deinococcus radiophilus

  • Oh, Kyung-A;Lee, Young-Nam
    • BMB Reports
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    • v.31 no.2
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    • pp.144-148
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    • 1998
  • A bifunctional catalase-peroxidase, designated catalase-2, of a UV resistant Deinococcus radiophilus was purified to electrophoretic homogeneity by both chromatographic and electrophoretic methods. Its molecular weight was 310 kDa and composed of a tetramer of 80 kDa subunits. The catalase-2 exerted its optimal activity at $30^{\circ}C$ and around pH 9. Its $K_m$ value for $H_{2}0_{2} $ was about 10 mM. It showed the typical ferric heme spectrum with maximum absorption at 403 nm which shifted to 419 nm in the presence of cyanide. The ratio of A40i' A2S0 was 0.48. Fifty percent inhibition of the enzyme activity was observed at $4.6{\times}10^{-6}$, $7.7{\times}10^{-6}$, and $3.0{\times}10^{-6}$ M of NaCN, $NaN_3$, and $NH_{2}OH$, respectively. The enzyme was thermostable and not sensitive to 3-amino-1,2,4-triazole. Treatment of the enzyme with ethanol-chloroform caused a partial loss (30%) of its activity. The catalase-2 was distinct from the Deinococcal bifunctional catalase-3 in a number of properties, particularly in its molecular structure and substrate affinity.

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Catalases in Acinetobacter sp. Strain JC1 DSM 3803 Growing on Glucose (포도당을 이용하여 성장하는 Acinetobacter sp. Strain JC1 DSM 3809에 존재하는 Catalase)

  • Shin, Kyoung-Ju;Ro, Young-Tae;Kim, Young-Min
    • Korean Journal of Microbiology
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    • v.32 no.2
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    • pp.155-162
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    • 1994
  • Cells of Acinetobacter sp. strain JC1 DSM 3803, an aerobic monoxide-oxidizing bacterium, growing on glucose exhibited high catalase activity at the mid-exponential growth phase. The enzyme activity decreased gradually after then until the early stationary phase, increased again at the mid-stationary phase, and then decreased again thereafter. Cells growing on glucose was found to contain three kinds of catalses. Cat1, Cat2 and Cat3. The activities of Cat1 and Cat3 did change significantly during growth, but that of Cat2 exhibited significant variation. Cat3 was found to present only in cells growing on glucose, but not in cells growing on carbon monoxide of methanol. The activities of call and Cat3 in cell-free extracts were stable upon treatment with ethanol and chloroform, but decreased to some extent when the enzymewere treated with 2mM $H_2O_2$ and/or 3-amino-1,2,4-triazole (AT). Cat2 was found to be extremely sensitive to the ethanol-chloroform and $H_2O_2$ treatments, but was insensitive to the AT treatment. Cat1 exhibited enzyme activity after incubation for 1 min at 80$^{\circ}C$. Cat2 and Cat3 did not show enzyme activity after incubation for 1 min at 60$^{\circ}C$ and 70$^{\circ}C$, respectively. Cat2 was found to have peroxidase activity. Cat3 was purified to homogenity in seven steps. The molecular weight of the native enzyme was estimated to be 150,000. Sodium dodecyl sulfate-gel electrophoresis revealed two identical subunits of molecular weight 65,000. The enzyme was found to show two $K_m$ values of 39 mM and 58mM. The optimal pH for the enzyme activity was 7.0, but the activities at pH 6.0, 8.0, and 9.0, were found to be comparable to that at the optimal pH. The optimal temperature for the enzyme activity was found to be 40$^{\circ}C$. The enzyme also exhibited strong activity at 20$^{\circ}C$, 30$^{\circ}C$, and 50$^{\circ}C$. The purified enzyme was not affected by the ethanol-chloroform treatment. The enzyme, howerver, showed less than 10% of the original activity when it was treated with 12 mN AT, 0.1 mM $NaN_3$ of 1mM KCN.

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Morphology Control of NTO Crystals with Various Recrystallization Techniques

  • Lee, H.Y.;K.K. Koo;Kim, K.J.;G.B. Lim;W.B. Jeong;Kim, S.H.;Kim, H.S.;Park, B.S.
    • Proceedings of the Korea Association of Crystal Growth Conference
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    • 1997.10a
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    • pp.123-127
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    • 1997
  • Various recrystallization techniques has been applied to control morphology and size of NTO(3-nitro-1, 2, 4-triazole-5-one) crystals. With cooling method, it was found that the size of NTO at aqueous solution was controlled in the range of 5 to 500 $\mu\textrm{m}$. The spherical or cubic shapes of particles were obtained by adjusting operating conditions. Hexagonal and cubic shaped crystals of NTO were also obtained by sonication and evaporative method using aqueous solution of NTO. Their particle sizes were ranged 20 to 30 $\mu\textrm{m}$. In gas anti-solvent method with NTO/DMF and NTO/DMSO solutions, cubic type of NTO was obtained and the range of their sizes was 0.5-2$\mu\textrm{m}$.

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Purification and characterization of catalase-3 of deinococcus radiophilus

  • Lee, In-Jeong;Lee, young-Nam
    • Journal of Microbiology
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    • v.33 no.3
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    • pp.239-243
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    • 1995
  • Deinococcus radiophilus, an UV resistant bacterium seemed to contain three issoenzymes of catalase. Among them, the samllest and most abundant species in cell-free extract, catalase-3 which also exhibited peroxidase activity was purified to electrophoretic homogeneity (145-fold purification) by chromatographic procedures. Its molecular weight was 155 kDa composed of four 38 kDa subunits. The $K_{m}$ value of catalase-3 for H$\_$2/O$\_$2/ was approximately 0.5 mM. This enzyme showed a typical ferric heme spectrum with maximum absorption at 405 nm. Upon binding to cyanide, the 405 nm peak shifted to 420 nm. Catalase-3 was very sensitive to inhibitors of heme proteins, such as cyanide, azide and hydroxylamine. A ratio of A$\_$405/A$\_$28O/ was 0.5 Catalase-3 was active over a wide range of pH, between pH 7 and 10. The enzyme was rather heat-labile and partially sensitive to edthanol-chloroform treatment, but resistant to 3-amino-1, 2, 4-triazole. Catalase-3 of D. radiophilus, which is a bifunction catalatic peroxidatic enzyme seemed to share certain molecular properties with the typical catalase and the catalase-[roxidase along with its own unique features.

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Complete Genome Sequence of Pseudarthrobacter sp. IC2-21, a Fluquinconazole-Degrading Soil Bacterium

  • Myoungjoo Riu;Songhwa Kim;Jaekyeong Song
    • Microbiology and Biotechnology Letters
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    • v.52 no.1
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    • pp.94-96
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    • 2024
  • Pseudarthrobacter sp. IC2-21 is isolated from the greenhouse soil in Icheon, Gyeonggi, Korea. This strain IC2-21 is a first fluquinconazole degrading soil bacterium. We analyze the whole genome sequence of Pseudarthrobacter sp. IC2-21. The sequence analysis revealed that Pseudarthrobacter sp. IC2-21 possesses a single 4,265,009 bps circular chromosome with a DNA G+C-content of 65.4%. This chromosome contains 3,942 protein-coding sequences and 12 rRNA and 51 tRNA genes. In the result of sequence analysis, it is revealed that strain IC2-21 possessed genes coding the triazole pesticides degradation related enzymes, such as oxygenase, and fluquinconazole degradation related genes.

Fabrication and Characterization of High Efficiency Green PhOLEDs with [TCTA-TAZ] : Ir(ppy)3 Double Emission Layers ([TCTA-TAZ] : Ir(ppy)3 이중 발광층을 갖는 고효율 녹색 인광소자의 제작과 특성 평가)

  • Shin, Sang-Baie;Shin, Hyun-Kwan;Kim, Won-Ki;Jang, Ji-Geun
    • Korean Journal of Materials Research
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    • v.18 no.4
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    • pp.199-203
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    • 2008
  • High-efficiency phosphorescent organic light emitting diodes using TCTA-TAZ as a double host and $Ir(ppy)_3$ as a dopant were fabricated and their electro-luminescence properties were evaluated. The fabricated devices have the multi-layered organic structure of 2-TNATA/NPB/(TCTA-TAZ) : $Ir(ppy)_3$/BCP/SFC137 between an anode of ITO and a cathode of LiF/AL. In the device structure, 2-TNATA[4,4',4"-tris(2-naphthylphenyl-phenylamino)-triphenylamine] and NPB[N,N'-bis(1-naphthyl)-N,N'-diphenyl-1,1'-biphenyl-4,4'-diamine] were used as a hole injection layer and a hole transport layer, respectively. BCP [2,9-dimethyl-4,7-diphenyl-1,10-phenanthroline] was introduced as a hole blocking layer and an electron transport layer, respectively. TCTA [4,4',4"-tris(N-carbazolyl)-triphenylamine] and TAZ [3-phenyl-4-(1-naphthyl)-5-phenyl-1,2,4-triazole] were sequentially deposited, forming a double host doped with $Ir(ppy)_3$ in the [TCTA-TAZ] : $Ir(ppy)_3$ region. Among devices with different thickness combinations of TCTA ($50\;{\AA}-200\;{\AA}$) and TAZ ($100\;{\AA}-250\;{\AA}$) within the confines of the total host thickness of $300\;{\AA}$ and an $Ir(ppy)_3$-doping concentration of 7%, the best electroluminescence characteristics were obtained in a device with $100\;{\AA}$-think TCTA and $200\;{\AA}$-thick TAZ. The $Ir(ppy)_3$ concentration in the doping range of 4%-10% in devices with an emissive layer of [TCTA ($100\;{\AA}$)-TAZ ($200\;{\AA}$)] : $Ir(ppy)_3$ gave rise to little difference in the luminance and current efficiency.

Conventional and Inverted Photovoltaic Cells Fabricated Using New Conjugated Polymer Comprising Fluorinated Benzotriazole and Benzodithiophene Derivative

  • Kim, Ji-Hoon;Song, Chang Eun;Kang, In-Nam;Shin, Won Suk;Zhang, Zhi-Guo;Li, Yongfang;Hwang, Do-Hoon
    • Bulletin of the Korean Chemical Society
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    • v.35 no.5
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    • pp.1356-1364
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    • 2014
  • A new conjugated copolymer, poly{4,8-bis(triisopropylsilylethynyl)benzo[1,2-b:4,5-b']dithiophene-alt-4,7- bis(5-thiophen-2-yl)-5,6-difluoro-2-(heptadecan-9-yl)-2H-benzo[d][1,2,3]triazole} (PTIPSBDT-DFDTBTz), is synthesized by Stille coupling polycondensation. The synthesized polymer has a band gap energy of 1.9 eV, and it absorbs light in the range 300-610 nm. The hole mobility of a solution-processed organic thin-film transistor fabricated using PTIPSBDT-DFDTBTz is $3.8{\times}10^{-3}cm^2V^{-1}s^{-1}$. Bulk heterojunction photovoltaic cells are fabricated, with a conventional device structure of ITO/PEDOT:PSS/polymer:$PC_{71}BM$/Ca/Al ($PC_{71}BM$ = [6,6]-phenyl-$C_{71}$-butyric acid methyl ester); the device shows a power conversion efficiency (PCE) of 2.86% with an open-circuit voltage ($V_{oc}$) of 0.85 V, a short-circuit current density ($J_{sc}$) of 7.60 mA $cm^{-2}$, and a fill factor (FF) of 0.44. Inverted photovoltaic cells with the structure ITO/ethoxylated polyethlyenimine/ polymer:$PC_{71}BM/MoO_3$/Ag are also fabricated; the device exhibits a maximum PCE of 2.92%, with a $V_{oc}$ of 0.89 V, a $J_{sc}$ of 6.81 mA $cm^{-2}$, and an FF of 0.48.

Synthesis and Biological Activities of Some New 3,6-Disubstituted 1,2,4-Triazolo[3,4-b]1,3,4-thiadiazole Derivatives

  • Rafiq, Muhammad;Saleem, Muhammad;Hanif, Muhammad;Maqsood, Muhammad Rizwan;Rama, Nasim Hasan;Lee, Ki-Hwan;Seo, Sung-Yum
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.3943-3949
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    • 2012
  • A series of aromatic hydrazides 3a-j were prepared by refluxing esters 2a-j with hydrazine hydrate in methanol, which were prepared by the esterification of 1a-j. Acetohydrazides 3a-j upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazate salts 4a-j, which on refluxing with hydrazine hydrate yielded substituted 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones 5a-j. The target compounds 6a-j were synthesized by condensing furan-3-carboxylic acid in the presence of polyphosphoric acid under reflux. The structures of newly synthesized compounds were characterized by IR, $^1H$ NMR, $^{13}C$ NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were screened for their urease, acetylcholine esterase inhibition, antioxidant and alkaline phosphatase inhibition activity. Almost all of the compounds 6a-j showed good to excellent activities against urease and acetylcholine esterase more than the reference drugs. Compounds 6f and 6g were more potent scavenger of free radicals than the reference n-propyl gallate. Compound 6b and 6h showed excellent activities of alkaline phosphatase as compare to the reference $KH_2PO_4$.

Efficacy of Uniconazole as a Phytoprotectant Against $SO_2$ Injury in Snap Bean (강남콩에 대한 $SO_2$ 피해경감제로서 uniconazole의 효과에 관한 연구)

  • ;Donald T. Krizek;Roman M. Mirecki;Edward H. Lee
    • Journal of Korean Society for Atmospheric Environment
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    • v.8 no.1
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    • pp.13-19
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    • 1992
  • This study was conducted to determine the efficacy of using uniconazole,[(E)-1-(4-chlorophenyl)-4,4-dimethyl-2-(1,2,4-triazole-1-yl)-1-penten-3-ol)] as a phytoprotectant against $SO_2$ injury in snap been (Phaseolus vulgaris L. 'Strike'). Thirteen days prior to $SO_2$ fumigation, plants were given a 100 ml soil drench of uniconazole solution at concentrations of 0.02, 0.10, 0.25 and 0.50 mg/pot. All four uniconazole concentrations were significantly effective in providing protection against $SO_2$ exposure(3 h at 1.5 ppm), but uniconazole treatment above 0.02 mg/pot severely reduced stem elongation, leaf enlargement, flowering date and pod number and weight. Uniconazole treatment had little or no effect on stomatal conductance but reduced transpiration rate on a whole plant basis by nearly 40%. This may reflect an alteration in canopy structure by reducing stem elongation and leaf enlargement. Although uniconazole did not increase the activities of superoxide dismutase(SOD) and peroxidase(POD) in non-$SO_2$-fumigated plants, it significantly increased those enzyme activities in $SO_2$-fumigated plants. Chlorophyll concentration on the basis of unit area was increased 50-60% by uniconazole. However, the difference was not detected on the basis of dry weight. $SO_2$ increased variable chlorophyll fluorescence (Fv) 48% after 1.5 h of exposure in non-uniconazole treated plants but decreased Fv in the plants after 3 h of exposure. By appliing uniconazole, it was possible to maintain high Fv values in the latter group of plants. These results suggest that the phytoprotective effects of uniconazole are related to its growth-retarding properties as an anti-gibberellin as well as the increase of activites of free radical scavengers such as SOD and POD.

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