• Title/Summary/Keyword: $C_2Cl_F_2$

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Pharmacokinetics of SD-0542, a Novel Histone Deacetylase Inhibitor, in Rats

  • Shin, Beom-Soo;Yoo, Sun-Dong
    • Journal of Pharmaceutical Investigation
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    • v.35 no.5
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    • pp.349-353
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    • 2005
  • This study reports the pharmacokinetics of a novel histone deacetylase inhibitor, SD-0542, in rats after i..v. and oral administration. SD-0542 was injected intravenously at doses of 10, 20, and 40 mg/kg. The terminal elimination half-life $(t_{1/2})$, systemic clearance (Cl), and steady-state volume of distribution $(V_{ss})$ remained unaltered as a function of dose, with their values ranging from 2.0-2.5 hr, 157.2-214.1 ml/min/kg, and 11.1-17.5 L/kg, respectively, whereas, the initial serum concentration $(C_0)$ and AUC increased linearly as the dose was increased. Renal excretion of SD-0542 was minimal. Oral pharmacokinetic studies were conducted in rats at a dose of 20 mg/kg. The $T_{max}$, Cl/F, $V_{z}/F$, and $t_{1/2}$ were 2.0 hr, 92864 ml/min/kg, 16331 L/kg, and 2.0 hr, respectively. Taken together, SD-0542 showed linear pharmacokinetics over the i.v. bolus dose range studied. SD-0542 was poorly absorbed, with the absolute oral bioavailability of 0.9%.

Synthesis of Cyclen-Based Copper Complexes as a Potential Estrogen Receptor Ligand (에스트로젠 수용체 리간드로서 사이클렌을 기본 구조로 한 구리 착물의 합성)

  • Park, Jeong-Chan;Pandya, Darpan N.;Jeon, Hak-Rim;Lee, Sang-Woo;Ahn, Byeong-Cheol;Lee, Jae-Tae;Yoo, Jeong-Soo
    • Nuclear Medicine and Molecular Imaging
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    • v.41 no.4
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    • pp.326-334
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    • 2007
  • Purpose: The estrogen receptor (ER), which is over-expressed in ER-positive breast tumors, has been imaged by positron emission tomography (PET) using $[^{18}F]$ labeled estrogen ligands, especially $[^{18}F]FES$. However, $[^{18}F]$ has relatively short-lived half-life ($t_{1/2}$ =1.8 h) and the labeling yield of radio-fluorination is usually low compared with $^{64}Cu\;(t_{1/2}=12.7\;h)$. 1,4,7,10-tetraazacyclododecane (cyclen) is used to form stable metal complexes with copper, indium, gallium, and gadolinium. With these in mind, we prepared cyclen-based Cu complexes which mimic estradiol in aspect of two hydroxyl groups. Materials and Methods: 1.7-Protected cyclen, 1.7-bis (benzyloxycarbonyl)-cyclen was synthesized according to the reported procedure. After introducing two 4-benzyloxybenzyl groups at 4,10-positions, the benzyloxycarbonyl and benzyl groups were removed at the same time by hydrogenation on Pd/C to give 1,7-bis(4-hydroxybenzyl)-1,4,7,10-tetraazacyclododecane (1). Results: The prepared ligand 1 was fully characterized by $^1H,\;^{13}C$ NMR, and mass spectrometer. The synthesized ligand was reacted with copper chloride and copper perchlorate to give copper complexes $[Cu(1)]^{2+}2(CIO_4^-)\;and\;[Cu(1)Cl]^+Cl^-$ which were confirmed by high-resolution mass (FAB). Conclusion: We successfully synthesized a cyclen derivative of which two phenol groups are located on trans position of N-atoms. And, two Cu(ll) complexes of +2 and +1 overall charge, were prepared as a potential PET tracers for ER imaging.

Stability of Tris(2-cyclohexylaminoethyl)amine-Zn(II) Complex (Tris(2-cyclohexylaminoethyl)amine-Zn(II) 착물의 안정성)

  • Yong Woon Shin;Hyun Sook Baek;Jae-Kyung Yang;Jineun Kim;Moo Lyong Seo
    • Journal of the Korean Chemical Society
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    • v.47 no.2
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    • pp.121-126
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    • 2003
  • Tris(2-cyclohexylaminoethyl)amine (L) was synthesized by the Schiff base condensation reaction of tris(2-aminoethyl)amine with cyclohexanone, followed by reduction. The thermodynamic characteristics, mole ratio and formation constant of [Zn(II)-L] complex were measured by the cyclic voltammetry and isothermal titration. In the case of Zn(II), well-defined cathodic and anodic peak were obtained at -1.02V and -0.48V vs Ag/AgCl , respectively. For the [Zn(II)-L] complex, both peaks were obtained at -1.19V and -0.45V vs Ag/AgCl, respectively. In addition, the peak height gradually increases as the scan rate increases, suggesting that the currents obtained were diffusion - controlled. The mole ratio and stability constant of the complex measured cyclic voltammerty were 1:1 and logK$_f$= 5.8, respectively. And the mole ratio and stability constant of the complexe calculated by isothermal titration method was 1:1 and logK =5.4, respectively. ${\Delta}$H, ${\Delta}$G and T${\Delta}$S for the complex formation were -53.0 kJ/mol, -31.1 kJ/mol, and -21.9 J/K at 25 ${\circ}$C, respectively.

Macroalkoxyamines and macroRAFT agents based on polyethylene for the syntheses of polyolefin based polar block copolymers

  • Lopez R. Godoy;Boisson C.;D'Agosto F.;Spitz R.;Boisson F.;Gigmes D.;Bertin D.
    • Proceedings of the Polymer Society of Korea Conference
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    • 2006.10a
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    • pp.377-377
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    • 2006
  • Alkoxyamine and thiocarbonyl thio end capped polyethylene (PE) chains were synthesized using a direct and simple approach consisting in reacting di(polyethylenyl)magnesium (PE-Mg-PE) chains with a range of nitroxides and disulfides of thiocarbonyl thio compounds. PE-Mg-PE compounds were prepared by a catalyzed chain growth reaction of ethylene on nbutyloctylmagnesium (BOMg) with a neodymocene complex $(C_{5}Me_{5})_{2}NdCl_{2}Li(OEt_{2})_{2}$. Complete characterizations confirm the introduction of the desired end groups. The controlled radical polymerization (NMP and RAFT) of butyl acrylate mediated by these functional polyethylenes was successful.

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A New Acetate Selective Polyamine Receptor Based on Anthracene and 4-Nitrophenyl Group

  • Lee, Sung-Kyu;Kang, Jong-Min
    • Bulletin of the Korean Chemical Society
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    • v.32 no.4
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    • pp.1228-1230
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    • 2011
  • A new amine receptor 2 utilizing anthracene and nitrophenyl group as signaling group was designed and synthesized. The receptor 2 only utilizes four amine N-H's and 9-anthracenyl hydrogen to bind anions. The receptor 2 can bind anions through hydrogen bonds with a selectivity of $CH_3CO_2^-$ > $H_2PO_4^-$ > $F^-$ > $C_6H_5CO_2^-$ > $Cl^-$ in highly polar solvent such as DMSO without protonation of amine.

Isolation and Cultivation of Microorganism Producing Levanbiose from Levan (Levan으로부터 Levanbiose를 생산하는 미생물의 분리 및 배양)

  • 이태호;강은정;강수경
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.27 no.3
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    • pp.441-447
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    • 1998
  • A bacterial strain No. 43 was isolated from soil samples as a levan-assimiating microorganism producing an extracellular levanase and hydrolying levan to levanbiose. According to the taxonomic characteristics of its morphological and physiological properties, the strain was idenified as Pseudomonas sp. No. 43. The optimum culura medium was composed of 10g levan, 5g(NH4)2SO4, 3g NH4Cl, 3g polypepton, 1g K2HPO4, 0.5gMgSO4.7H2O, and 0.2g MnCl2.4H2O per liter. The cultivation for levanase was carried out in pH 7.0 at 4$0^{\circ}C$ for 28hr. The reaction product was a kind of oligosaccharide and it was purified by chilled ethanol precipitation and gel filtration for evalluation of degree of polymerization (DP). The purified product was determined as levanbiose of MW 342 and DP2 by HPLC and FAB-MS.

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Bond Orbital Theory of Chemical Reactivity (反應性의 結合 Orbital 理論)

  • Yang, Kang;Ree, Tai-Kyue
    • Journal of the Korean Chemical Society
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    • v.8 no.1
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    • pp.20-24
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    • 1964
  • The linear combination of bond orbitals method is used to investigate the reactivity of halomethanes in abstraction reactions by atoms. The activation energy is evaluated on the assumption that, in an activated complex, two electrons in a bond to be broken become completely isolated from the rest of the ${\sigma}$-electron systems. Such a model leads to an intuitively attractive concept that the interactions between the reactive bond and the neighboring bonds govern the reactivity of ${\sigma}$-electron systems. The resulting equation for the activation energy, ${\varepsilon},\;is:\;{\narepsilon}= ${\varepsilon}={\zeta}+$$${\sum}_{i=1}^3$${\eta}c-I,$ c-4 Here, subscript C-4 indicates the bond to be broken, while C-i represents the other three bonds surrounding the reactive bond; ξ is the activation energy of a hypothetical reaction of an isolated C-4 bond and an attacking atom; and ${\eta}$C-i,C-4 stems from the stabilizing interacting of C-4 bond with neighboring C-i bonds. A choie of η′s consistent with bond strength data simplifies the above equation to a form ${\varepsilon}={\zeta}\;+\;N{\eta}c$-H, C-4 where N denotes the number of C-H plus C-F bond in halomethanes. In agreement with this equation, experimental -values increase linearly with increasing N.

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The Recycling of Inorganic Industrial Waste in Cement Industry (시멘트산업에서 무기질 산업 폐·부산물의 재활용)

  • Kang, S.K.;Nam, K.U.;Seo, H.N.;Kim, N.J.;Min, K.S.;Chung, H.S.;Oh, H.K.
    • Clean Technology
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    • v.6 no.1
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    • pp.61-69
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    • 2000
  • In this study, generation process and properties of inorganic industrial waste which can be used in cement industry were investigated. The scheme of recycling to use the selected waste as raw materials, mineralizer and flux, admixture and raw materials for special cement was decided and then various experiments were carried out. The experimental results were as follows ; In the use of industrial waste as raw materials, ferrous materials could be substituted by Cu-slag, Zn-slag, electric arc furnace or convertor furnace slag etc., and a siliceous material could be substituted by sand from cast-iron industry. By-products from sugar or fertilizer industry, which has $CaF_2$ as the main component, and jarosite from Zn refinery enabled clinker phases to be formed at lower temperature by $100{\sim}150^{\circ}C$. Adding Cu slag and STS sludge in proper proportion to cement improved properties of cement. Fly ash and limestone powder as admixture had the same effect on cement. As a raw material for special cement, aluminium waste sludge could be used in making ultra early strength cement, which had the compressive strength of $300kg/cm^2$ within 2hours. And two different ashes from municipal incinerator could be raw materials of the cement which was mainly composed of $C_3S$ and $C_{11}A_7{\cdot}CaCl_2$ as clinker phases.

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Effect of Neutral Salts on the Reactive Dyeing of Silk (Ⅱ) - Effect of Anions - (중성염이 견의 반응염색에 미치는 영향 (Ⅱ) - 음이온의 영향 -)

  • Do, Seong Guk;Park, Chan Heon;Gwon, Ji Yun
    • Textile Coloration and Finishing
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    • v.13 no.2
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    • pp.28-28
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    • 2001
  • Four kinds of neutral sodium salts with different anions, NaF, NaCl, NaBr, and NaI, were added to the dye bath to accurately understand the effect of anions on the reactive dyeing of silk with C. I. Reactive Black 5. The sodium cation lowered the negative surface potential of the silk and increased the dye-uptake on fille fabric as reported previously. However, because of the discrepancy in the anions′inhibition power from cation′s lowering the surface negative potential the amount of the dye on the silk fiber was different from each other in the order of $F^-\;>\;Cl^-\;>\; Br^-\;>\;I^-$. The activation energy($E_a$) for the dyeing was in the order of $F^-\;>\;Cl^-\;>\; Br^-\;>\;I^-$ but the dye-uptake on the fabric and the activation free energy(Δ$G^*$), the real energy barrier for the reaction, were in the order of $F^-\;>\;Cl^-\;>\; Br^-\;>\;I^-$ because the strength of the interaction of the anions with sodium cations was the same as the order of the latter. In other words $F^-$ exerted the weakest electrostatic force on $Na^+$and competed with the dyestuff anions least of all. The decrease in Δ$S^*$may be due to the looesly bonded activated complex of dyestuff anions, sodium cations and fiber molecules at transition state. It was clarified from the Bronsted equation that sodium salts with different anions also had fille ionic strength effect and the specific salt effect on the reactive dyeing.

The Wrinkle Resistance and DP Rating of Tencel Treated with BTCA (BTCA를 이용한 텐셀의 방추성 및 DP성)

  • 양인영;송화순
    • Journal of the Korean Society of Clothing and Textiles
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    • v.28 no.910
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    • pp.1265-1272
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    • 2004
  • The purpose of this study is to develope wrinkle recovery property, DP rating of Tencel by using BTCA(1,2,3,4-butanetetracarboxylic acid) and MgCl$_2$ that does not make water pollution. The adoptable condition to improve the wrinkle resistance and DP rating was determined 10% BTCA(o.w.f), 3% catalyst(o.w.f), 0.5% softener(o.w.f), 5min padding time, 150$^{\circ}C$ curing temperature, 2min curing time and pH 2.7. It was proven that ester groups were formed and cross-links increased by treating Tencel with BTCA. By XPS diffraction, Tencel treatment using BTCA was proved not to affect crystal formation.