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

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Activity Profiles of Linear, Cyclic Monomer and Cyclic Dimer of Enkephalin

  • Kim, Dong-Hee;Hong, Nam-Joo
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.261-269
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    • 2012
  • The cyclic dimers of enkephalin were isolated as minor components during the solution synthesis of the corresponding cyclic monomers. The ratio of cyclic dimer to monomer was approximately 1:4 from the percent of yields. In the receptor binding assay of two cyclic dimmers, ($Tyr_2-C[D-Glu-Phe-gPhe]_2$ 6, $Tyr_2-C[D-Asp-Phe-gPhe-rLeu]_2$ 8), both analogs exhibited the high preference for ${\delta}$ receptor compared to monocyclic counterparts. In the nociceptive activity, both showed about 5 times less potent than the cyclic monomers. The repeated synthesis of 14-membered cyclic analog, Tyr-C[D-Glu-Phe-gPhe-D-rLeu] 14, which was known as having three distinct cis-trans isomers, gave rise to apparently different conformational analog arousing only trans isomer. In the receptor binding assay, it showed tremendously high selectivity toward ${\mu}$ receptor $({\delta}/{\mu}=160)$.

Synthesis of New 6-(4-Fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b] thiazole Derivatives and their Antiproliferative Activity against Melanoma Cell Line

  • Park, Jin-Hun;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.31 no.10
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    • pp.2854-2860
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    • 2010
  • Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).

Synthesis and Evaluation of Cytotoxicity of Novel Arylsulfonylimidazolidinones Containing Sulfonylurea Pharmacophore

  • Jung, Sang-Hun;Song, Jae-Shin;Lee, Hui-Soon;Choi, Sang-Un;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.570-580
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    • 1996
  • Design and synthesis of novel 4-phenyl-1-arylsulfonylimidazolones 3 and 4-phenyl-3-arylsulfonylimidazolones 4 and evaluation of their cytotoxic activity against eleven human cancer cell lines and two murine leukemia cell lines in vitro were performed. As a result, a series of 4-phenyl-1(N)-arylsulfonylimidazolones (3) has been found to be the potential anticancer agent. Compounds 3b, 3c, and 3d exhibit strong activity as indicated by their $IC_{50}$ values 0.39, 3.19, $0.31{\mu}g/mL$ against A549 and 0.80, 0.48, $0.0007{\mu}g/mL$against SK-Mel-2, respectively. These compounds also possess much more potent activity (10-1000 times) than LY186641 against eleven other cell lines.

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Synthesis and Sintering of Cordierite from Metal Alkoxides(I) -Synthesis of Cordierite from Metal Alkoxides- (금속 Alkoxide로부터 Cordierite 분말의 합성 및 소결에 관한 연구(I) -금속 Alkoxide로부터 Cordierite분말의 합성-)

  • 한문희;박금철
    • Journal of the Korean Ceramic Society
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    • v.27 no.5
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    • pp.625-630
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    • 1990
  • Cordierite powders were prepared from Si(OC2H5)4, Al(OC3H7i)3 and Mg(OC2H5)2 by the sol-gel method. Two different methods were applied for producing fine and homogeneous powders. One is that Si(OC2H5)4 with a lowr rate of hydrolysis was partially hydrolyzed and then Al(OC3H7i)3 and Mg(OC2H5)2 were mixed and reacted. The other is based on the simultaneous hydrolysis of these metal alkoxides using i-C4H9OH which retards the rate of hydrolysis of Al(OC3H7i)3 and Mg(OC2H5)2. It was confirmed that ifne and homogeneous powders were obtained from both methods. Also these powders were calcined at four different temperatures during two hours. X-ray diffraction patterns show only ${\mu}$-cordierite phase at 1000$^{\circ}C$, ${\mu}$-cordierite and ${\alpha}$-cordierite phases at 1100-1200$^{\circ}C$ and ${\alpha}$-cordierite phase at 1300$^{\circ}C$ respectively.

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Robust Hcontrol applied on a fixed wing unmanned aerial vehicle

  • Uyulan, Caglar;Yavuz, Mustafa Tolga
    • Advances in aircraft and spacecraft science
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    • v.6 no.5
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    • pp.371-389
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    • 2019
  • The implementation of a robust $H_{\infty}$ Control, which is numerically efficient for uncertain nonlinear dynamics, on longitudinal and lateral autopilots is realised for a quarter scale Piper J3-Cub model accepted as an unmanned aerial vehicle (UAV) under the condition of sensor noise and disturbance effects. The stability and control coefficients of the UAV are evaluated through XFLR5 software, which utilises a vortex lattice method at a predefined flight condition. After that, the longitudinal trim point is computed, and the linearization process is performed at this trim point. The "${\mu}$-Synthesis"-based robust $H_{\infty}$ control algorithm for roll, pitch and yaw displacement autopilots are developed for both longitudinal and lateral linearised nonlinear dynamics. Controller performances, closed-loop frequency responses, nominal and perturbed system responses are obtained under the conditions of disturbance and sensor noise. The simulation results indicate that the proposed control scheme achieves robust performance and guarantees stability under exogenous disturbance and measurement noise effects and model uncertainty.

Control of Flexible Link using Mixed $H_2$/H$\infty$ and $\mu$-Synthesis Method

  • Y.W. Choe;Lee, H.K.;J.I. Bae
    • 제어로봇시스템학회:학술대회논문집
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    • 2001.10a
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    • pp.95.3-95
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    • 2001
  • This paper investigates the simultaneous use of mixed H2/H_inf and mu-synthesis design methodology to design a robust controller for flexible link. We adopt four steps to design control system as follows: Step 1 : Generally, there are differences between the nominal and real model, so we consider the plant as a combination of parametric model uncertainty and unstructured uncertainty represents real structural uncertainties associated with the damping ratios of the flexible modes retained in the nominal model without payload. denotes the uncertainty which is due to the payload added at the tip. Step 2 : We adopt the mixed H2/H_inf theory to design a feedback controller K(s) by using the model uncertainty ...

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A Study on the Hydrothermal Synthesis of Clay Mineral (II) -Hydrothermal Synthesis of Clay Mineral from Anorthite in San.Chung District of Korea- (수열반응에 의한 인공점토의 합성연구 (II) -경남 산청산 회장석으로부터 인공점토의 수열합성에 관한 연구-)

  • 이응상;이상훈
    • Journal of the Korean Ceramic Society
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    • v.32 no.6
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    • pp.735-747
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    • 1995
  • The synthesis of clay mineral through the hydrothermal reaction of the anorthite, which is distributed in San Chung-District of Korea and called as the ground rock for halloysite-kaolin, has been investigated. It was observed that this anorthite sample was easily converted into clay mineral with 0.5 wt% HCl solution at a temperature below 20$0^{\circ}C$ under a pressure about 15 atm. The conversion reaction was promoted by adding aluminum chloride under the condition concerned. Aluminum chloride was considered to supply the insufficient aluminum ion during the conversion reaction and to reprepare the acid solution-condition by adding the HCl-component as a by-product. According to the electron micrographs, it was confirmed that fine tubular or needle-shaped halloysite-kaolin minerals with the crystal length shorter than about 1.1${\mu}{\textrm}{m}$ could be obtained by the hydrothermal reaction for 5 days under those conditions.

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Synthesis of Kaolinite and Transformation of Halloysite byHydrothermal Reaction (열수반응에 의한 Kaolinite의 합성 및 Halloysite의 개질)

  • 김성규;이화영;오종기
    • Journal of the Korean Ceramic Society
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    • v.30 no.1
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    • pp.41-45
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    • 1993
  • synthesis of artificial kaolinite and the transformation of domestic halloysite have been attempted by means of the hydrothermal treatment. The hydrothermal reaction of the mixtures of gibbsite and amorphous silica was conducted for the synthesis of kaolinite under the pressure of 125MPa at 30$0^{\circ}C$ and especially the seed of kaolinite was added so as to facilitate the synthesis reaction. Domestic pink kaolin of B-grade was hydrothermally treated, in a similar way, for the transformation of crystalline form of it. Boehmite and the artificial kaolinite less than 0.4${\mu}{\textrm}{m}$ could be obtained through the hydrothermal reaction. It could also be found that the majority of hyalloysite was transformed into the plate-type kaolinite through the recrystallization by treating hydrothermally for a long time.

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Response of Muscle Protein Synthesis to the Infusion of Insulin-like Growth Factor-I and Fasting in Young Chickens

  • Kita, K.;Shibata, T.;Aman Yaman, M.;Nagao, K.;Okumura, J.
    • Asian-Australasian Journal of Animal Sciences
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    • v.15 no.12
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    • pp.1760-1764
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    • 2002
  • In order to elucidate the physiological function of circulating IGF-I on muscle protein synthesis in the chicken under malnutritional conditions, we administrated recombinant chicken IGF-I using a osmotic mini pump to fasted young chickens and measured the rate of muscle protein synthesis and plasma metabolite. The pumps delivered IGF-I at the rate of $22{\mu}g/d\{300{\mu}g{\cdot}(kg\;body\;weight{\cdot}d)^{-1}\}$. Fractional rate of protein synthesis in the muscle was measured using a large dose injection of L-[$2,6-^3H$]phenylalanine. Constant infusion of chicken IGF-I did not affect plasma glucose level. Significant interaction between dietary treatment and IGF-I infusion was observed in plasma NEFA and total cholesterol concentrations. When chicks were fasted, IGF-I infusion decreased plasma NEFA and total cholesterol concentrations. On the other hand, IGF-I administration did not affect plasma levels of both metabolites. Fasting reduced plasma triglyceride concentration significantly. IGF-I infusion also decreased the level of plasma triglyceride. Plasma IGF-I concentration of young chickens was halved by fasting for 1 d. IGF-I infusion using an osmotic minipump for 1 d increased plasma IGF-I concentration in fasted chicks to the level of fed chicks. Fasting decreased body weight and the loss of body weight was significantly ameliorated by IGF-I infusion. There was a significant interaction between dietary treatment and IGF-I infusion in the fractional rate of breast muscle protein synthesis. There was no effect of IGF-I infusion on muscle protein synthesis in fed chicks. Muscle protein synthesis reduced by fasting was ameliorated by IGF-I infusion, but did not reach to the level of fed control. Muscle weight of fasted chicks infused with IGF-I was similar to fasted birds without IGF-I infusion, which suggests that muscle protein degradation would be increased by IGF-I infusion as well as protein synthesis in fasted chicks.