• Title/Summary/Keyword: $\mu$ synthesis

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Synthesis of Selective Butyrylcholinesterase Inhibitors Coupled between α-Lipoic Acid and Polyphenols by Using 2-(Piperazin-1-yl)ethanol Linker

  • Yeun, Go Heum;Lee, Seung Hwan;Lim, Yong Bae;Lee, Hye Sook;Won, Moo-Ho;Lee, Bong Ho;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • v.34 no.4
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    • pp.1025-1029
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    • 2013
  • In the previous paper (Bull. Korean Chem. Soc., 2011, 32, 2997), the hybrid molecules between ${\alpha}$-lipoic acid (ALA) and polyphenols (PPs) connected with neutral 2-(2-aminoethoxy)ethanol linker (linker-1) showed new biological activity such as butyrylcholinesterase (BuChE) inhibition. In order to increase the binding affinity of the hybrid compounds to cholinesterase (ChE), the neutral 2-(2-aminoethoxy)ethanol (linker 1) was switched to the cationic 2-(piperazin-1-yl)ethanol linker (linker 2). The $IC_{50}$ values of the linker-2 hybrid molecules for BuChE inhibition were lower than those of linker-1 hybrid molecules (except 9-2) and they also had the same great selectivity for BuChE over AChE (> 800 fold) as linker-1 hybrid molecules. ALA-acetyl caffeic acid (10-2, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.44{\pm}0.24{\mu}M$). A kinetic study using 7-2 showed that it is the same mixed type inhibition as 7-1. Its inhibition constant (Ki) to BuChE is $4.3{\pm}0.09{\mu}M$.

Synthesis and Structure Dinitroethylenediamine Palladium(II) (Dinitroethylenediamine Palladium(II)의 합성 및 결정구조 연구)

  • Namgung Hae
    • Korean Journal of Crystallography
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    • v.15 no.2
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    • pp.74-77
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    • 2004
  • The crystal structure of Dinitroethylenediaminepalladium(II), $Pd(C_2H_8N_2)(NO_2)_2$, has been determined by X-ray crystallography. Crystal data: a=7.425(3), b=8.480(4), c=11.885(2) ${\AA}$, Orthorhombic, $A2_1ma$ (Space Group No=36), Z=4, V=748.3(4) ${\AA}^3,\;D_c=2.295 gcm^{-3},\;{\mu}=2.457mm^{-1}$. The structure was solved by Patterson method and refined by full matrix least-square methods using unit weights. The final R and S values were $R_1=0.0306,\;R_w=0.0802,\;R_{all}=0.0320,\;and\;S=1.166)$ for the observed 377 reflections. Bond lengths and angles of palladium complex are similar to the previously reported data. The complex structure is one dimensional Reiset's salt type analogue showing zigzag chain of Pd-Pd length and angle of 3.762(2) ${\AA}$ and $161.41(5)^{\circ}$. The complex molecules are linked through inter-and intramolecular hydrogen bonds of 3.05(1) and 3.15(1) ${\AA}$ between oxygen and nitrogen.

Synthesis and Crystal Structure of $Me_2Pt(PPh_2CH_2C(t-Bu)=N-N=CMe(2-py)-\kappa^2N,P)$ ($Me_2Pt(PPh_2CH_2C(t-Bu)=N-N=CMe(2-py)-\kappa^2N,P)$의 합성 및 결정 구조)

  • Cho Sung Il;Kang Sang Ook;Chang K.
    • Korean Journal of Crystallography
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    • v.15 no.2
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    • pp.83-87
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    • 2004
  • An organometallic complex. $Me_2Pt(PPh_2CH_2C(t-Bu)=N-N=CMe(2-py)-\kappa^2N,P)$ was synthesized from phosphinohydrazone $Ph_2PCH_2C(t-Bu)=NNH_2$, 2-acetylpyridine, and $[PtMe2({\mu}-SMe_2)]_2$. The molecular structure of this complex has been determined by X-ray diffraction. Crystallographic data: monoclinic, space group $P2_1/n,\;a=11.6926(7)\;{\AA},\;b=15.6607(19)\;{\AA},\; c=14.6125(6)\;{\AA},\;\beta=93.018(4)^{\circ},\;Z=4,\;V=2672.0(4)\;{\AA}^3$. The structure was solved by direct methods and refined by full-matrix least-squares methods to give a model with a reliability factor R = 0.0363 for 5238 reflections.

Synthesis and Evaluation of Antitumor Activity of Novel 1,4-Naphthoquinone Derivatives (IV)

  • Kim Bok Hee;Yoo Jikang;Park Si-Hyun;Jung Jae-Kyung;Cho Hoon;Chung Yongseog
    • Archives of Pharmacal Research
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    • v.29 no.2
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    • pp.123-130
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    • 2006
  • 1,4-Naphthoquinones are widely distributed in nature and many clinically important antitumor drugs containing a quinone moiety, such as anthracyclines, mitoxantrones and saintopin, show excellent anticancer activity. In this study, 2- or 6-substituted 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) and 5,8-dihydroxy-1,4-naphthoquinone (DHNQ) derivatives were synthesized, and their cytotoxic activity against L1210 and P388 cancer cells was examined. Their antitumor activity was also assessed in mice bearing S-180 cells in the peritoneal cavity. In comparison with the DMNQ derivatives, the DHNQ derivatives exhibited more potent bioactivities than the DMNQ derivatives against both L1210 and P388 cells in vitro and S-180 cells in vivo. The $ED_{50}$ values of the DHNQ derivatives against P388 cells were in the range of 0.18-1.81 ${\mu}g/mL$ whereas those of the DMNQ derivatives were in the range of 0.26-40.41 ${\mu}g/mL$. The T/C ($\%$) values of the DHNQ derivatives, 8, 17, 18, 19, and 20, were found to be comparable to or even better than that of adriamycin. It was also observed that the 2-substituted derivatives (8, 19, 20) showed better antitumor activity than the 6-substituted derivatives (7, 17, 18) in the mice bearing S-180 cells in the peritoneal cavity.

Synthesis and Smooth Muscle-Selective Relaxant Activity of a Piperidine Analogue: 1-(4'-Fluorophenacyl)-4-Hydroxy-4-Phenyl-Piperidinium Chloride

  • Taqvi, Syed Intasar Hussain;Ghayur, Muhammad Nabeel;Gilani, Anwarul Hassan;Saify, Zafar Saeed;Aftab, Mohammad Tariq
    • Archives of Pharmacal Research
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    • v.29 no.1
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    • pp.34-39
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    • 2006
  • The antispasmodic and vasodilator activities of a newly synthesized piperidine derivative (1-(4'fluorophenacyl)-4-hydroxy-4-phenyl-piperidinium chloride) were studied in vitro. The test compound exhibited a dose-dependent relaxant effect on the spontaneous and $K^+$ (75 mM)-induced contractions of isolated rabbit jejunum with respective $EC_{50}$ values of 0.01 mM(0.01-0.02, 95% CI) and 0.30 mM (0.17-0.56). The $Ca^{++}$ channel blocking (CCB) activity was confirmed when the test compound (0.1-0.2 mM) shifted the $Ca^{++}$ dose-response curves to the right, similar to that produced by verapamil ($0.1-1.0{\mu}M$), a standard CCB. In the isolated rabbit aorta, the test compound showed a dose-dependent vasodilator effect on $K^+$ (75 mM)-induced contractions with an $EC_{50}$ value of 0.08 mM (0.02-0.26) while also suppressed the norepinephrine ($1{\mu}M$) control peak responses with $EC_{50}$ value of 0.08 mM (0.05-0.13, n=5). When tested in Langendorff perfused rabbit heart preparation, the test compound exhibited a negligible inhibitory effect on the rate or force of atrial and ventricular contractions when tested up to 5 mM. The results show smooth muscle-selective relaxant effect of the test compound on intestinal and vascular preparations mediated possibly via blockade of voltage and receptor-operated $Ca^{++}$ channels.

Synthesis of Electrolyte Films for Low-Temperature Solid Oxide Fuel Cells by Sol-Gel Coating and Their Characteristics (졸-겔 코팅에 의한 저온형 고체산화물 연료저지용 전해질막의 합성 및 특성)

  • 현상훈;김승구;장운석
    • Journal of the Korean Ceramic Society
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    • v.36 no.4
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    • pp.391-402
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    • 1999
  • Characteristics of composite electrolytes which were prepared by coating a thin film of YSZ (yttria sta-bilized zirconia : (ZrO2)0.92 (Y2O3)0.08) on YDC (yttria doped ceria : Ce0.8Y0.2O1.9) with mixed conductivity have been investigated in order to develop the low-temperature solid oxide fuel cell. The thickness (t) of spin-coated YSZ thin films after the heat-treatment at 600$^{\circ}C$ was increased proportionally to the sol con-centrations (C) while the decrease in its thickness with the spin rate ($\omega$) could be expressed in the e-quation of ln t=9.49-0.53 ln $\omega$(0.99mol//s sol conc.) When the sol concentration and the spin rate being less than 0.99 mol/l and higher than 1000 rpm respectively reliable YSZ/YDC composite electrolytes could be obtained by multi-coating although several micro-cracks were observed in singly coated YSZ film surfaces. The dense YSZ film with a 1$\mu\textrm{m}$ thickness was prepared by coating of 0.99 mol/l YSZ sol five-times at 2000 rpm followed by heat-treatment at 1400$^{\circ}C$ for 2h, The adhesion between YSZ film and YDC substrate was found to be very good. The open circuit voltages of H2/O2 single cell with YSZ/YDC composite electrolytes were 0.79∼0.82 V at 800$^{\circ}C$ and 0.75∼0.77V at 900$^{\circ}C$ The open circuit voltage was inversely proportioned to the thickness ratio of YSZ thin film (1$\mu\textrm{m}$) to YDC substrate(0.28-2.22 mm)

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An Area-efficient Design of SHA-256 Hash Processor for IoT Security (IoT 보안을 위한 SHA-256 해시 프로세서의 면적 효율적인 설계)

  • Lee, Sang-Hyun;Shin, Kyung-Wook
    • Journal of the Korea Institute of Information and Communication Engineering
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    • v.22 no.1
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    • pp.109-116
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    • 2018
  • This paper describes an area-efficient design of SHA-256 hash function that is widely used in various security protocols including digital signature, authentication code, key generation. The SHA-256 hash processor includes a padder block for padding and parsing input message, so that it can operate without software for preprocessing. Round function was designed with a 16-bit data-path that processed 64 round computations in 128 clock cycles, resulting in an optimized area per throughput (APT) performance as well as small area implementation. The SHA-256 hash processor was verified by FPGA implementation using Virtex5 device, and it was estimated that the throughput was 337 Mbps at maximum clock frequency of 116 MHz. The synthesis for ASIC implementation using a $0.18-{\mu}m$ CMOS cell library shows that it has 13,251 gate equivalents (GEs) and it can operate up to 200 MHz clock frequency.

Development of the Frequency Synthesizer for Multi-function Radar (다기능 레이더용 주파수합성기 개발)

  • Yi, Hui-min;Choi, Jae-hung;Han, Il-tak
    • Journal of the Korea Institute of Information and Communication Engineering
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    • v.22 no.8
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    • pp.1099-1106
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    • 2018
  • In this paper, we developed and then analyzed the specifications of the frequency synthesizer which was applied to long range MFR (Multi-function Radar). These specifications were able to guarantee the functions and performance of MFR. MFR was the radar system that used phase array for electronically scanning. This frequency synthesizer made various frequency signals including to STALO (Stable Local Oscillator) for MFR. By analyzing the MFR requirements, we choose the optimal frequency synthesis method and then we got the best performance and functionality including to physical size for this system. We designed and fabricated DDS (Direct Digital Synthesizer)-driven Offset-PLL (Phase Locked Loop) synthesizer to meet the requirements which were low phase noise, fast switching time and low spurious. This synthesizer had less than -131dBc/Hz@100kHz phase noise and less than $4.1{\mu}s$ switching time, respectively.

Preparation of Zinc Oxide by Hydrothermal Precipitation and Degradation of Tartrazine (수열 합성법에 의한 Zinc Oxide의 제조 및 Tartrazine 분해 특성)

  • Na, Seok-Eun;Jeong, Sang-Gu;Jeong, Ga-Seop;Kim, Si-Young;Ju, Chang-Sik
    • Korean Chemical Engineering Research
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    • v.49 no.6
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    • pp.752-757
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    • 2011
  • The effects of reaction temperature, reactant concentration, pH of solution and mixing order of reactants on the particle shape and size distribution of zinc oxide were investigated in the preparation of zinc oxide from ammonium hydroxide and zinc acetate by the method of aqueous hydrothermal precipitation method, and the photocatalytic ability of zinc oxide synthesized was measured from the degradation of tartrazine under UV irradiation. The average particle size was increased with pH of solution but decreased with zinc acetate concentration and reaction temperature. The optimum condition for the synthesis of minimum sized zinc oxide was pH 11.2, concentration of zinc acetate 0.6 M and reaction temperature $90^{\circ}C$, and its average particle size was 3.133 ${\mu}$m. 97% of tartrazine was degraded by zinc oxide in sixty minutes.

Effect of Ponciri Fructus Extracts Fermented with Ganoderma lucidum on the Collagen Synthesis and Expression of Matrix Metalloproteinase-1 (콜라겐 합성과 MMP-1 발현에 대한 생물전환 지실 추출물의 효과)

  • Lee, Gye Won;Park, Sung Min;Yoo, Yung Choon;Cho, Young Ho
    • KSBB Journal
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    • v.28 no.2
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    • pp.106-114
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    • 2013
  • Ponciri fructus, the unripe fruits of Poncirus trifoliata, are widely used in oriental traditional medicine as a remedy for inflammation, gastritis, emesis, digestive ulcers, allergy, and dysentery. To study the anti-wrinkle effects of Ponciri fructus extract (PFE) containing flavanone glycosides, PFE was fermented with Ganoderma lucidum mycelia and its biological activities were investigated. In Ponciri fructus extracts fermented with G. lucidum (G-PFE), polyphenol content was $1,021.00{\pm}0.50{\mu}g/mL$ and flavonoid content was $589.41{\pm}0.21{\mu}g/mL$. G-PFE was found to scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and superoxide anion radical by a dose dependent manner, respectively. G-PFE showed higher antioxidant activity than that of PFE. In addition, the photoprotective properties of G-PFE was tested in human dermal fibroblasts (HDF) exposed to UVA radiation. G-PFE inhibited the activity of matrix metalloproteinase-1 (MMP-1) and showed a dose dependent decrease in the expression level of MMP-1. G-PFE also increased collagen biosynthesis in HDF. These results demonstrate that G-PFE could be useful as a potential cosmetic ingredient for anti-wrinkle.