• Title/Summary/Keyword: elemental substitution

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Synthesis and Anticonvulsant Evaluation of N-Substituted-Isoindolinedione Derivatives

  • Abdel-Hafez, Atef Abdel-Monem
    • Archives of Pharmacal Research
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    • v.27 no.5
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    • pp.495-501
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    • 2004
  • A series of N-substituted-1,3-isoindolinedione derivatives (2-16) were synthesized for the purpose of defining the effect of N-substitution on the anticonvulsant activity of these derivatives. The target compounds (2-16) were obtained by condensation of phthalic anhydride with the corresponding amine derivative. The structures of the synthesized derivatives (2-16) were confirmed by means of IR, $^1$H-NMR, $^{13}$ C-NMR, MS and elemental analyses. The anticonvulsant activity of all compounds (2-16) were evaluated by subcutaneous pentylenetetrazole seizure threshold test at doses of 0.2, 0.4 and 0.8 mmol/kg compared with sodium valproate as a positive control. Their neurotoxicity were determined by the rotorod test. Many of the present series of compounds showed good anticonvulsant activity at the tested doses, as compared to sodium valproate. Three of them (4, 6 and 11) exhibited 100 % protection against convulsions, neurotoxicity and death at all tested doses. Out of the series, two compounds (12 and 13) were completely inactive with 100% mortality. 3-(p-chlorophenyl)-4-(1 ,3-dioxo-2,3-dihydro-1 H-2-isoindolyl) butanoic acid derivative (11) has emerged as the most active compound which is 20 times more active than valproate with ED$_{50}$ 8.7, 169 mg/kg; TD$_{50}$ 413, 406 mg/kg and PI 47.5, 2.4. The results revealed the importance of the combination of baclofenic and phthalimide moieties (compound 11) as a promising anticonvulsant candidate.

PREPARATION OF POLYSTYRENE BEADS CONTAINING SULFONAMIDE GROUPS AND THEIR APPLICATION TO POLYMERIC BIOCIDES

  • Kim, Cheol-Jin;Kim, Jee-Yeon;Byun, Jang-Woong;Kim, Jae-Eun;Lee, Yoon-Sik;Yoon, Je-Yong
    • Environmental Engineering Research
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    • v.11 no.6
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    • pp.325-332
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    • 2006
  • A novel series of polystyrene (PS) beads containing various sulfonamide groups was prepared, and their chemical stabilities in an aqueous solution were tested in order to determine their ability to inactivate microbes. By reacting aminomethyl polystyrene (AM PS) beads or carboxy polystyrene beads with various benzenesulfonic acid derivatives, the sulfonamide groups were introduced on the PS beads. The characteristics of the product beads were analyzed by elementary analysis after the substitution of various sulfonamide groups. Energy Dispersive Spectroscopy (EDS), and FT-IR analysis were used to analyze the elemental functional group composition, respectively. The hydrolytic stabilities of the PS beads containing various sulfonamide groups along with the relationship between the swelling ratio and their hydrophilicity were investigated. The antibacterial activity of the beads was determined by their ability to inactivate E. coli. This study reports that PS beads containing sulfonamide groups had lasting antibacterial efficacy over a satisfactory period, whilst maintaining their chemical stabilities against hydrolysis. The 8 synthesized polymer beads exhibited antibacterial ability.

Magnetic Properties of Mn and La-Mn Substituted Strontium Ferrite (Mn 및 La-Mn 치환 Sr 페라이트의 자기적 특성 변화)

  • 장세동;김종오;김종희
    • Journal of the Korean Magnetics Society
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    • v.11 no.6
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    • pp.267-271
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    • 2001
  • These experiments were carried out to examine the effects of elemental substitution of Mn and La-Mn on Sr-ferrite. The calcined properties for the Mn and La-Mn substitution were examined, and the sintered magnetic properties were compared with the stoichiometric condition. The magnetic properties of calcined SrM and (La-Mn)$_{0.3}$-SrM composition were as follows, respectively; M$_{s}$ : 61.06 emu/g, $_{i}$H$_{c}$ : 4.45 kOe and M$_{s}$ : 61.06 emu/g, $_{i}$H$_{c}$ : 4.46 kOe. Also, the sintered ferrite magnets of Mn$_{0.3}$-SrM and [(La-Mn)$_{0.3}$-SrM exhibited a similar properties to the stoichiometric composition but the coercivity of (La-Mn)$_{x}$-SrM was decreased rapidly with x=0.5.

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Production of $[^{18}F]F_2$ Gas for Electrophilic Substitution Reaction (친전자성 치환반응을 위한 $[^{18}F]F_2$ Gas의 생산 연구)

  • Moon, Byung-Seok;Kim, Jae-Hong;Lee, Kyo-Chul;An, Gwang-Il;Cheon, Gi-Jeong;Chun, Kwon-Soo
    • Nuclear Medicine and Molecular Imaging
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    • v.40 no.4
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    • pp.228-232
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    • 2006
  • Purpose: electrophilic $^{18}F(T_{1/2}=110\;min)$ radionuclide in the form of $[^{18}F]F_2$ gas is of great significance for labeling radiopharmaceuticals for positron omission tomography (PET). However, its production In high yield and with high specific radioactivity is still a challenge to overcome several problems on targetry. The aim of the present study was to develop a method suitable for the routine production of $[^{18}F]F_2$ for the electrophilic substitution reaction. Materials and Methods: The target was designed water-cooled aluminum target chamber system with a conical bore shape. Production of the elemental fluorine was carried out via the $^{18}O(p,n)^{18}F$ reaction using a two-step irradiation protocol. In the first irradiation, the target filled with highly enriched $^{18}O_2$ was irradiated with protons for $^{18}F$ production, which were adsorbed on the inner surface of target body. In the second irradiation, the mixed gas ($1%[^{19}F]F_2/Ar$) was leaded into the target chamber, fellowing a short irradiation of proton for isotopic exchange between the carrier-fluorine and the radiofluorine absorbed in the target chamber. Optimization of production was performed as the function of irradiation time, the beam current and $^{18}O_2$ loading pressure. Results: Production runs was performed under the following optimum conditions: The 1st irradiation for the nuclear reaction (15.0 bar of 97% enriched $^{18}O_2$, 13.2 MeV protons, 30 ${\mu}A$, 60-90 min irradiation), the recovery of enriched oxygen via cryogenic pumping; The 2nd irradiation for the recovery of absorbed radiofluorine (12.0 bar of 1% $[^{19}F]fluorine/argon$ gas, 13.2 MeV protons, 30 ${\mu}A$, 20-30 min irradiation) the recovery of $[^{18}F]fluorine$ for synthesis. The yield of $[^{18}F]fluorine$ at EOB (end of bombardment) was achieved around $34{\pm}6.0$ GBq (n>10). Conclusion: The production of $^{18}F$ electrophilic agent via $^{18}O(p,n)^{18}F$ reaction was much under investigation. Especially, an aluminum gas target was very advantageous for routine production of $[^{18}F]fluorine$. These results suggest the possibility to use $[^{18}F]F_2$ gas as a electrophilic substitution agent.

Novel Syntheses of 5-Aminothieno[2,3-c]pyridazine, Pyrimido[4',5':4,5]thieno[2,3-c]pyridazine, Pyridazino[4',3':4,5]thieno-[3,2-d][1,2,3]triazine and Phthalazine Derivatives

  • El Gaby, Mohamed S.A.;Kamal El Dean, Adel M.;Gaber, Abd El Aal M.;Eyada, Hassan A.;Al Kamali, Ahmed S.N.
    • Bulletin of the Korean Chemical Society
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    • v.24 no.8
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    • pp.1181-1187
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    • 2003
  • Condensation of 4-cyano-5,6-dimethyl-3-pyridazinone 1 with aromatic aldehydes gave the novel styryl derivatives 2a-c. Refluxing of compound 2a with phosphorus oxychloride furnished 3-chloropyridazine derivative 3. Compound 3 was reacted with thiourea and produced pyridazine-3(2H)thione 4. Thieno[2,3-c]- pyridazines 5a-e were achieved by cycloalkylation of compound 4 with halocompounds in methanol under reflux and in the presence of sodium methoxide. Also, refluxing of compound 4 with N-substituted chloroacetamide in the presence of potassium carbonate afforded thienopyridazines 6a-e. Cyclization of compound 6 with some electrophilic reagents as carbon disulfide and triethyl orthoformate furnished the novel pyrimido[4',5':4,5]thieno[2,3-c]pyridazines 12 and 13a-c, respectively. Diazotisation of compound 6 with sodium nitrite in acetic acid produced the pyridazino[4',3':4,5]thieno[3,2-d][1,2,3]triazines 14a-c. Ternary condensation of compound 1, aromatic aldehydes and malononitrile in ethanol containing piperidine under reflux afforded the novel phthalazines 16a-c. Compound 3 was subjected to some nucleophilic substitution reactions with amines and sodium azide and formed the aminopyridazines 17a, b and tetrazolo[1,5-b]-pyridazine 19, respectively. The structures of the synthesized compounds were established by elemental and spectral analyses.

Preparation of High Range Water Reducer Containing Carboxylic Acid and Their Cement Absorptivity(I) (카르본산계 고성능감수제의 제조 및 그들의 시멘트 흡착성(I))

  • 김화중;강인규;김성훈;김우성;권영도
    • Magazine of the Korea Concrete Institute
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    • v.7 no.2
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    • pp.175-182
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    • 1995
  • Styrene-Maleic anhydride copolymer (SMA) was prepared by the radical copolmerization of styrene and maleic anhydride using ${\alpha}-{\alpha}'$ azobis(isobutyronitrile) as an initiatrr. SMA was further reacted with m-amino phenol to obtain aminophenol-substituted SMR (mSMA). Sulfonated SMA and mSMA were also prepared by the reaction of copolymers with sulfuric acid The copolyniers were characterized by infrared spectroscopy. It was found from the results of elemental analysis that the substitution degree of aminophenol in the mSMR is 44% and the degree is lowered to 35% after sulfonation. The percentage of copolymers adsorbed on the surface of cement particles was increased with a decrease of added copolymers. While, the arnourit of sulfonated SMA absorbed on the surface of cement particles was larger than that of the sulfonated mSMA The copolymers synthesized in this study are probably expected as a high range water reducer for coiicxte.

Solubility of Liquid Crystalline Hydroxypropyl Chitin in Organic Solvent (액정성 히드록시프로필키틴의 유기용매에 대한 용해성)

  • Lee, Young Moo;Kim, Seong Soo;Kim, Seon Jeong;Sung, Yong Kiel;Kang, In Kyu;Son, Tae II
    • Applied Chemistry for Engineering
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    • v.4 no.2
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    • pp.403-408
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    • 1993
  • Hydroxypropyl chitin(HPCH) was prepared from chitin by reacting it with propylene oxide. The formation of liquid crystalline character of HPCH was investigated using halogenated organic solvents. Solid state $^{13}C$ NMR spectra for chitin and HPCH confirmed the incorporation of hydroxypropyl moiety. The degree of substitution of HPCH was around 0.8 as detected by elemental analysis. WAXD patterns of chitin and HPCH showed that an incorporation of hydroxypropyl unit in chitin contributed to reducing the crystallinity and enhancing the solubility in organic solvents. Polarized light microscopic pictures of concentrated HPCH solution showed that HPCH formed cholesteric liquid crystalline character at about 25w/v% solution in dichloroacetic acid and 1, 2-dichloroethane. Inherent viscosity of HPCH solution in a mixed solvent showed a transient decrease.

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Thermoelectric Properties of Skutterudite FexCo4-xSb12 Synthesized by Mechanical Alloying Process (기계적 합금화에 의한 Skutterudite계 FexCo4-xSb12의 합성 및 열전특성)

  • Kwon, Joon-Chul;Kim, Il-Ho;Ur, Soon-Chul
    • Journal of Powder Materials
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    • v.12 no.5 s.52
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    • pp.357-361
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    • 2005
  • Fe-doped skutterudite $CoSb_3$ with a nominal composition of $Fe_{x}Co_{4-x}Sb_{12}(0\;{\le}\;x\;{\le}\;2.5)$ has been synthesized by mechanical alloying (MA) of elemental powders, followed by hot pressing. Phase transformations during mechanical alloying and hot pressing were systematically investigated using XRD. Single phase skutterudite was successfully produced by vacuum hot pressing using as-milled powders without subsequent annealing. However, second phase in the form of marcasite structure $FeSb_2$ was found to exist in case of $x\;{\ge}\;2$, suggesting the solubility limit of Fe with Co in this system. Thermoelectric properties as functions of temperature and Fe contents were evaluated for the hot pressed specimens. Fe substitution up to x=1.5 with Co in $Fe_{x}Co_{4-x}Sb_{12}$ appeared to increase thermoelectric figure of merit (ZT) and the maximum ZT was found to be 0.78 at 525K in this study.

Adsorption of uranium(VI) ion on the nitrogen-donor macrocyclic synthetic resin adsorbent (질소-주게 거대고리 합성수지 흡착제에 의한 우라늄(VI) 이온의 흡착)

  • Kim, Joon-Tae
    • Analytical Science and Technology
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    • v.21 no.2
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    • pp.109-116
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    • 2008
  • Resins were synthesized by mixing 1-aza-18-crown-6 macrocyclic ligand into styrene(dangerous matter) divinylbenzene(DVB) copolymer with crosslink of 1%, 2%, 6% and 12% by substitution reaction. The synthesis of these resins was confirmed by content of chlorine, elemental analysis, thermogravimetric analysis, electron microscopy, and IR. The effects of pH, time, crosslink of resins and dielectric constant of solvent on adsorption of uranium ion by resin adsorbent were investigated. Uranium ion showed a great adsorption above pH 3 and adsorption equilibrium of metal ions was established in about two hours. In addition, adsorptive selectivity of resin in ethanol solvent was $UO{_2}^{2+}$ > $Zn^{2+}$ > $Lu^{3+}$ ion and adsorption of uranium ion increased with the increase of the degree of crosslinking (1%~12%) and was inversely in proportional to the order of dielectric constant of solvents.

A close look at the influence of praseodymium (III) oxide on the structural, physical, and γ-ray protection capacity of a ternary B2O3-PbO-CdO glass system

  • R.H. Shoeir;M. Afifi;Abdelghaffar S. Dhmees;M.I. Sayyed;K.A. Mahmoud
    • Nuclear Engineering and Technology
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    • v.56 no.6
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    • pp.2258-2265
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    • 2024
  • The present investigation aims to study the role of Pr2O3 on the structural, physical, and radiation shielding properties of a dense cadmium lead borate glass. The XRD was used to affirm the glassy amorphous structure of fabricated sample materials. Moreover, the FTIR was used to record the change in the FT-IR spectra due to the addition of Pr2O3 in the wavenumber interval between 400 and 4000 cm-1. The features of glass surfaces and the elemental analyses for the synthesized Pr2O3-reinforced cadmium lead borate glasses were performed using a SEM, supported by an energy-dispersive spectrometer. The γ-ray protection capacity was evaluated using the Monte Carlo method in a wide energy interval ranging between 0.015 and 15 MeV. The linear attenuation coefficient (LAC) at 1 MeV was reduced by a factor of 10 % from 0.372 cm-1 to 0.340 cm-1. The decrease in the LAC values negatively affected the other shielding properties such as half-value thickness and the transmission factor. Although the linear attenuation coefficient is decreased slightly with the partial substitution of CdO by Pr2O3 compound, the fabricated glass samples still have a high shielding capacity compared to the traditional commercial glasses as well as previous similar reported glasses.