• Title/Summary/Keyword: Oxime

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In vitro Screening of Oxime Reactivators on the Model of Paraoxon-inhibited Acetylcholinesterase-SAR Study

  • Holas, Ondrej;Musilek, Kamil;Pohanka, Miroslav;Kuca, Kamil;Opletalova, Veronika;Jung, Young-Sik
    • Bulletin of the Korean Chemical Society
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    • v.31 no.6
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    • pp.1609-1614
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    • 2010
  • Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Standard in vitro test was chosen using a rat brain homogenate as the source of AChE. Screening of reactivation potency was performed with two concentration of reactivator (1000 ${\mu}M$ and 10 ${\mu}M$). Results were compared to established reactivators pralidoxime, methoxime, HI-6, trimedoxime and obidoxime. More than 30 novel reactivators performed equal or better reactivation ability of POX-inhibited AChE compared to currently used reactivators. The structure-activity relationship for reactivators of paraoxon-inhibited AChE was developed.

Copper(II), Nickel(II) and Palladium(II) Complexes of 2-Oximino-3-thiosemicarbazone-2,3-butanedione

  • Al-Kubaisi, Abdulla H.
    • Bulletin of the Korean Chemical Society
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    • v.25 no.1
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    • pp.37-41
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    • 2004
  • A new tridentate ligand incorporating a monoxime and thiosemi-carbozone moieties has been synthesized. Its copper(II), nickel(II) and palladium(II) complexes have been prepared and characteirzed by physical and spectral methods. Elemental analyses and spectroscopic data of the metal complexes are consistent with the formation of a mononuclear copper(II) complex and binuclear complex with both nickel(II) and palladium(II). In the copper(II) complex the fourth coordination site is occupied by nitrate ion. In the binculear complexes the fourth coordination site is occupied by the deprotonated oxime oxygen of the ligand coordinated to the other metal.

Determination of $\alpha$--pyrrolidone in panax ginseng Extracts (인삼 extract중의 $\alpha$-pyrrolidone검정)

  • 서정상
    • YAKHAK HOEJI
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    • v.13 no.4
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    • pp.111-120
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    • 1969
  • The determination of $\alpha$-pyrrolidone in ginseng extract by gas liquid chromatography (GLC) was established. $\alpha$-Pyrrolidone in extract was tentatively identified by comparison of the relative retention time of sample peak with those of reference compound and coinjection noted peak enhancement. The .alpha.-pyrrolidone peak elimination was demonstrated by formation of oxime when treated with excess of NH$_{2}$OH ${\cdot}$ HCl and NaOH, allowed to stand at room temperature for 5 minute. The elimination was also observed when samples were treated by the same procedure. The above method was proved to be useful for the determination of $\alpha$-pyrrolidone in ginseng extract and in ginseng extract mixed with 51 plant extracts.

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Physical Properties of Octahedral Iron (Ⅱ) Complexes of Vicinal-Dioximes (팔면체형 철 (Ⅱ) Vicinal-디옥심 착물의 물리적 성질)

  • Chong-Shik Chin;L. Vaska
    • Journal of the Korean Chemical Society
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    • v.24 no.5
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    • pp.380-392
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    • 1980
  • Six coordinate low spin iron(Ⅱ) complexes of vicinal-dioximes, [Fe$(DH)_2B_2$] and [Fe$(DH)_2$B(CO)]($(DH)_2$=$(CHDH)_2$(bis(1,2-cyclohexadinedioximato) bivalent anion), $(DPGH)_2$-(bis(diphenylglyoximato) bivalent anion), $(F{\alpha}DH)_2(bis(furil-{\alpha}-dioximato)$ bivalent anion); B = monodentate neutral nitrogen base), have been prepared and their physical properties have been investigated with respect to the effects of the equatorial ligands, $(DH)_2$. The order of ${\pi}$-acceptor CO stretching frequency for [Fe$(DH)_2$B(CO)] is $(F{\alpha}DH)_2$ > $(DPGH)_2$> $(CHDH)_2$, while non-${\pi}$-acceptor $NH_3$ stretching frequencies for [Fe$(DH)_2(NH_3)_2$] show the opposite order to that of CO, i.e., $(CHDH)_2$ > $(DPGH)_2$ > $(F{\alpha}DH)_2$. These infrared spectral data together with Fe-N (oxime) and Fe-N (oxime) and Fe-N (B) stretching frequency data suggest that the nitrogen atoms of $(CHDH)_2$ are more basic and poorer ${\pi}$-acceptors than the corresponding nitrogen atoms of $(DPGH)_2$ and $(F{\alpha}DH)_2$, respectively. It has been found from the electronic spectral data of [Fe$(DH)_2$] and [Fe$(DH)_2$B(CO)] that the energy of the charge transfer band from iron(Ⅱ) to $(DH)_2$ increases as the basicity of $(DH)_2$ increases.

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The Effects of Ethanol on Cholinesterase Inactivation by Organophosphorous (에탄올이 유기인제 농약에 의한 Cholinesterase 불활성화에 미치는 영향)

  • Choi, Hyoung-Chul;Kim, Jong-Ho;Ha, Jeoung-Hee;Lee, Kwang-Yoon;Kim, Won-Joon;Woo, Hyun-Jae;Huh, Chang-Uk;Son, Soo-Min;Chun, Eun-Jin
    • Journal of Yeungnam Medical Science
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    • v.16 no.2
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    • pp.326-332
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    • 1999
  • Background: In korea the agricultural community widely uses organophosphorous, and organophosphorous poisonings are increasing every year. We compared change in activity of acetylcholinesterase and pseudocholinesterase by organophosphorous and by the interaction of ethanol and organophosphorous. We also compared the effect of reversible anticholinesterase drugs, physostigmine and neostigmine The object of this study is to investigate the effects of several anticholinesterase drugs and on how ethanol influences the activity of cholinesterase. Materials and Methods: Fifteen male university students were randomly selected, and blood samples were taken from the antecubital vein. The acetylcholinesterase in the RBC and the pseudocholinesterase in the serum were extracted and separated. The enzyme activity change was measured by the electrometric method. After adding acetylcholine, the pH change was measured with a pH meter. Results and Conclusion: Our results indicated that reversible anticholinesterase drugs decreased the cholinesterase activity more efficiently than organophosphorous. The acetyl cholinesterase and pseudocholinosterase activity were decreased by ethanol. When ethanol was added, oxime a cholinesterase activator, increased acetylcholinesterase activity but does not increased pseudocholinesterase activity.

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Analysis of Formaldehyde and Acetaldehyde in Alcoholic Beverage (유통 주류의 포름알데히드 및 아세트알데히드 함량분석)

  • Park, Young-Seok;Lee, Yun-Jeung;Lee, Ki-Teak
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.35 no.10
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    • pp.1412-1419
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    • 2006
  • Concentrations of formaldehyde and acetaldehy de were respectively analysed in forty-five alcoholic beverages obtained from the market. After derivatization with PFBHA, GC-ECD and GC-MSD were employed for analysis. The peak area of aldehyde oximes (derivatives with PFBHA) increased with the increasing ethanol content (5%, 10%, 15%, 20% and 40%). When three-point calibration corves for the selected ethanol concentration (5, 13, 21 and 40%, v/v) were studied, suitable linearity against ethanol concentration was observed only under 5, 13, and 21% (ethanol, v/v). After analysis, maximum content of formaldehyde (average of 0.272 ppm) and acetaldehyde (average of 15.262 ppm) among the observed 45 alcoholic beverages was found from whisk (2 species) while minimum content of formaldehyde (average of 0.009 ppm) and acetaldehyde (average of 0.805 ppm) was found from diluted soju (4 species).

In vitro Evaluation of New Acetylcholinesterase Reactivators as Casual Antidotes against Tabun and Cyclosarin

  • Kuca, Kamil;Jun, Daniel;Kim, Tae-Hyuk;Cabal, Jiri;Jung, Young-Sik
    • Bulletin of the Korean Chemical Society
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    • v.27 no.3
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    • pp.395-398
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    • 2006
  • Nerve agents (sarin, tabun, soman and VX) are class of military important substances able to cause many severe intoxications during few minutes. Currently, the threat of misuse of these agents is daily discussed. Unfortunately, there is no single antidote able to treat intoxication caused by all of these agents. Owing to this fact, new generation of antidotes, especially acetylcholinesterase (AChE; EC 3.1.1.7) reactivators, is still developed. In this study, we have tested four newly developed AChE reactivators: 1-(4-hydroxyiminomethylpyridinium)- 5-(4-carbamoylpyridinium)-3-oxa-pentane dibromide (1), 1-(3-hydroxyiminomethylpyridinium)-5-(4-carbamoylpyridinium)-3-oxa-pentane dibromide (2), 1,5-bis(2-hydroxyiminomethylpyridinium)-3-oxa-pentane dichloride (3) and 1,5-bis(4-hydroxyiminomethylpyridinium)-3-oxa-pentane dibromide (4) for their potency to reactivate in vitro tabun and cyclosarin-inhibited AChE. Their reactivation efficacy was compared with currently the most promising oxime HI-6 (1-(2-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-2-oxa-propane dichloride). According to obtained results, two AChE reactivators 1 and 4 were able to reactivate tabun-inhibited AChE. On the contrary, there was no better AChE reactivator than HI-6 able to reactivate cyclosarin-inhibited AChE.

Catalytic and Structural Properties of Pyridoxal Kinase

  • Cho, Jung-Jong;Kim, Se-Kwon;Kim, Young-Tae
    • BMB Reports
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    • v.30 no.2
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    • pp.125-131
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    • 1997
  • This work reports studies of the catalytic and structural properties of pyridoxal kinase (ATP: pyridoxal 5' -phosphotransferase, EC. 2.7.1.35), Pyridoxal kinase catalyzes the phosphorylation of vitamin $B_6$ (pyridoxal, pyridoxamine, pyridoxine) using ATP-Zn as a phosphoryl donor. The enzyme purified from brain tissues is made up of two identical subunits of 40 kDa each. Native enzyme was inhibited by a substrate analogue, pyridoxal-oxime. Limited chymotrypsin digestion of pyridoxal kinase yields two fragments of 24 and 16 kDa with concomitant loss of catalytic activity. These fragments were isolated by DEAE ion exchange chromatography and used for binding studies with fluorescent ATP and pyridoxal analogues. The spectroscopic properties of both fluorescent pyridoxal analogue and Anthraniloyl ATP (Ant-ATP) bound to the 24 kDa fragment are indistinguishable from those of both pyridoxal analogue and Ant-ATP bound to the native pyridoxal kinase, respectively. The small 16 kDa fragment, generated by proteolytic cleavage of the kinase, does not bind any of the substrate analogues. Binding characteristics of Ant-ATP were extensively studied by measuring the changes in fluorescence spectra at various conditions. From the results presented herein, it is postulated that the structural domain associated with catalytic activity comprises approximately one-half of the molecular mass of pyridoxal kinase (24 kDa). whereas the remaining portion (16 kDa) of the enzyme contains a regulatory binding domain.

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Recovery of Copper from Spent Copper Solution of Printed Circuit Board Process by Solvent Extraction Method (인쇄회로기판 제조과정에서 발생되는 동폐액의 용매추출에 의한 재활용)

  • Moon, Young-Hwan
    • Clean Technology
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    • v.2 no.1
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    • pp.47-52
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    • 1996
  • The solvent extraction method was applied on a spent solution containing copper, which was produced in a printed circuit board process, to recover copper and to reuse the etching solution. Lix 64 N ($\alpha$-Hydroxyoxime + $\beta$-Hydroxybenzophenone Oxime) was used as a solvent. The acidic spent copper solution was mixed with and alkaline copper solution to pH=2. The solvent including 30 volume% of Lix 64 N extracted 17.1gr/l of copper from the mixed spent copper solution. In the continuous bench scale experiment, 4 stages for extraction, 2 stages for stripping and 4 stages for washing were used. Recovered copper was recycled as copper sulfate and the raffinate was reused as copper etchant. The percentage of copper recovery and the purity of copper sulfate were higher than 99.9%, respectively.

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