• Title/Summary/Keyword: ring opening

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Pharmacological Activities of Flavonoids (I) -Relationships of Chemical Structure of Flavonoids and their Inhibitory Activity of Hypersensitivities- (Flavonoids의 약리작용(I) -Flavonoids 구조와 과민반응 억제작용과의 상관성-)

  • Kim, Chang-Johng;Chung, Jin-Mo
    • YAKHAK HOEJI
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    • v.34 no.5
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    • pp.348-364
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    • 1990
  • The activities of twenty-one flavonoids and their related compounds on the hypersensitivity reaction against various antigens were studied in vitro and in vivo. 1. Generally flavonoids inhibited significantly the homologous passive cutaneous anaphylaxis (PCA) induced by reaginic antibody as compared as anaphylaxis by compound 48/80-induced mast cell degranulation, and so more strongly active in the IgE-mediated anaphylaxis than non-IgE-mediated anaphylaxis. 2. Flavonids inhibited remarkably Arths reaction, hemolysin titer, delayed hypersensitivity, haemagglutinin titer, rosette forming cells and plague forming cells against sheep red blood cells, and so it exhibited that flavonoids inhibited type 2, 3 and 4 hypersensitivity. 3. Quercetin, kaempferol, hesperetin, disodium cromoglycate, malvin and baicalein were active dose-dependently in the all types of hypersensitivity. Fisetin, daidzein, morin, narigin, flavone, catechin, rutin, hesperidin, neophsperidin, apigenin and chrysin were significantly active in the various types of hypersensitivity, but apigenin, rutin and catechin were less active in the delayed hypersensitivity. Taxifolin was significantly active in PCA and histamine-induced anaphylaxis except other types of hypersensitivity. Rotenone and cyanin also inhibited all types of hypersensitivity, but they are toxic. 4. Based on these results from hypersensitivity, the following flavonoid structure-activity relationships became apparent. 1) Flavonoids with $C_{2-3}$ double bond in C-ring were more active than that of $C_{2-3}$ saturation. 2) Flavonoids with $C_4$ ketone group in C-ring were more active than abscence of them except catechin and malvin. 3) Flavonoids with benzene ring at positions 2 or 3 in C-ring exhibited same activities. 4) Flavonoids with opening of the C-ring does not abolish their activities. 5) The glycosylated flavonoids in position 3 or 7 was less active than their aglycone. 6) Flavonoids with the more hydroxy group in A and B-ring were more active. 7) Flavonoids with or without $C_3-OH$ did not change their activities.

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Development of On-line Control System Using RFID On the Prison (RFID를 이용한 교도소의 온라인 통제 시스템 개발)

  • Park, Seung-Hwan;Ku, Ja-Yl
    • 전자공학회논문지 IE
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    • v.45 no.4
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    • pp.74-79
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    • 2008
  • The paper represented central management system of dual direction that does opening and shutting, real-time check of various doors of the prison in the on-line network. To remove a fault of 125kHz RFID technology, we use 13.56MHz RFID technology, can solve the problem of the maintenance and trust, development of on-line control and management system that ring the alarm in the abnormal opening and shutting doors.

An Open Bridcage RF coil for Magnetic Rresonance Imaging (자기공명영상을 위한 개방형 새장 고주파코일)

  • Lee, S.Y.;Yi, J.H.;Yi, W.;Mun, C.W.;Cho, M.H.
    • Journal of the Korean Institute of Telematics and Electronics S
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    • v.35S no.5
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    • pp.42-47
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    • 1998
  • Bridcage RF coil is one of the most widely used RF coils in MRI. In order to use birdcage RF coils in open MRI systems, an open tructured birdcage RF coil has been investigated. By opening the ring structure of an original birdcage RF coil and driving the coil at two opening ends, the original birdcage RF coil can be modified to an open structured coil. In order to improve magnetic field uniformity of the open birdcage RF coil, driving voltage phases at the two opening ends can be controlled to be in-phase or out-of-phase each other. Operating frequency of the open birdcage RF coil has been theoretically derived, and the theoretical derivation has been verified by experiments.

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Synthesis and Characterization of Biodegradable MethoxyPoly(ethylene glycol)-Poly$(\varepsilon-caprolactone-co-L-lactide)$ Block Copolymers (메톡시폴리(에틸렌 글리콜)-폴리(카프로락톤-co-L-락타이드) 공중합체의 합성 및 특성 분석)

  • Hyun Hoon;Cho Young Ho;Jeong Sung Chan;Lee Bong;Kim Moon Suk;Khang Gilson;Lee Hai Bang
    • Polymer(Korea)
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    • v.30 no.1
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    • pp.28-34
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    • 2006
  • A series of methoxypoly(ethylene glycol) $(MPEG)-poly(\varepsilon-co-L-lactide)$ (PCLA) diblock copolymers were synthesized by ring-opening polymerization of a mixture of $\varepsilon-caprolactone$ and L-lactide with different ratios in the presence of $Sn(Oct)_2$. The characterization of MPEG-PCLA diblock copolymers were examined by $^1H-NMR$, GPC, DSC, and XRD. Kinetic study on ring-opening polymerization of monomer mixtures was carried out in various conditions such as a variation with polymerization time, amount of catalyst, and temperature. The highest conversion obtained in 1.2 ratic of initiator venn catalyst at $110\;^{\circ}C$. The biodegradable characterization of MPEG-PCLA diblock copolymers in aqueous solution was carried out by using GPC for $1\~14$ weeks. The biodegradability of MPEG-PCLA diblock copolymers increased as the L-lactide content of diblock copolymers increased. In conclusion, we confirmed the dependence of polymerization rate according to various conditions. In addition, we can control the biodegradability of MPEC-PCLA diblock copolymers by changing the ratio of PCL and PLA block segment.

Synthesis of Methoxy Poly(ethylene glycol)/Polyesters Diblock Copolymers and Evaluation of Micellar Characterization as Drug Carrier (메톡시 폴리(에틸렌 글리콜)/폴리에스테르 블록공중합체의 합성 및 미셀 특성 비교)

  • Hyun, Hoon;Yang, Jae-Chan;Kim, Moon-Suk;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.30 no.6
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    • pp.464-470
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    • 2006
  • Diblock copolymers consisting of methoxy Poly (ethylene glycol) (MPEG) and poly (${\epsilon}-ca$ prolactone) (PCL), poly(${\delta}-valerolactone$) (PVL), poly(L-lactide) (PLLA), or poly(L-lactide-co-glycolide) (PLGA) were prepared to compare the characterization of diblock copolymers as a drug carrier. MPEG-PCL, MPEG-PVL, MPEG-PLLA, and MPEG-PLGA diblock copolymers were synthesized by the ring-opening polymerization of ${\epsilon}$-caprolactone or ${\delta}$-valerolactone in the presence of $HCl{\cdot}Et_2O$ as a monomer activator at room temperature and by the ring-opening polymerization of L-lactide or a mixture of L-lactide and glycolide in the presence of stannous octoate at $130^{\circ}C$, respectively. The synthesized diblock copolymers were characterized with $^1H-NMR$, GPC, DSC, and XRD. The micellar characterization of MPEG-polyester diblock copolymers in an aqueous phase was carried out by using NMR, dynamic light scattering, AFM, and fluorescence techniques. Most micelles exhibited a spherical shape in AFM. Thus, ore confirmed that the micelles formed with MPEG-polyester diblock copolymers have possibility as a potential hydrophobic drug delivery vehicle because a hydrophobic drug could be preferentially distributed in the micelle core.

The Base-Catalysed Carbonato or Oxalato Ring Opening of $cis-{\beta}-$$[Co(3,2,3-tet)(CO_3 or C_2O_4)]^+$ (3,2,3-tet=4,7-diazadecane-1,10-diamine) (염기성 촉매에 의한 $cis-{\beta}-$$[Co(3,2,3-tet)(CO_3 or C_2O_4)]^+$ (3,2,3-tet=4,7-diazadecane-1,10-diamine)에 대한 Carbonato 혹은 Oxalato 리간드의 고리열림 반응)

  • Yoon, Doo Cheon;Oh, Chang Eon;Kim, Bok Jo;Doh, Myung Ki
    • Journal of the Korean Chemical Society
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    • v.40 no.7
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    • pp.501-508
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    • 1996
  • The base-catalysed carbonato or oxalato ring opening of cis-${\beta}-[Co(3,2,3,-tet))CO_3\;or\;C_2O_4)]^+$(3,2,3-tet=4,7-diazadecane-1,10-diamine, $C_2O_4$=oxalate) has been investigated in aqueous solution and in mixed aqueous-organic solvent. The rearrangement of 3,2,3-tet and carbonato or oxalato ring opening of cis-${\beta}-[Co(3,2,3,-tet))CO_3\;or\;C_2O_4)]^+$ occurred via the dissociation of one of the two coordinating carbonato or oxalato oxygen atoms. The resulting product was cis-${\alpha}-[Co(3,2,3-tet)(OH)(OCO_2\;or\;OC_2O_3)_3].$ It has been suggested that the base-catalysed reaction of cis-${\beta}-[Co(3,2,3,-tet))CO_3\;or\;C_2O_4)]^+$ takes place via the Dcb(dissociative conjugated base) mechanism. The other oxygen atom of carbonato or oxalato was dissociated continuously to give cis-${\alpha}-[Co(3,2,3-tet)(OH)_2]^+.$ Cis-${\alpha}-[Co(3,2,3-tet)(OH)_2]^+$ was isomerized to cis-${\beta}-[Co(3,2,3-tet)(OH)_2]^+.$

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Synthesis of Thermosensitive and Biodegradable Methoxy Poly(ethylene glycol)-Polycaprolactone and Methoxy Poly(ethylene glycol)-Poly(lactic acid) Block Copolymers (온도감응 및 생분해성 폴리에틸렌 글리콜-폴리카프로락톤과 폴리에틸렌 글리콜-폴리락타이드 공중합체의 합성)

  • 서광수;박종수;김문석;조선행;이해방;강길선
    • Polymer(Korea)
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    • v.28 no.3
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    • pp.211-217
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    • 2004
  • The sol to gel transition of aqueous solution of block copolymers consisting of methoxy poly (ethylene glycol) (MPEG) and biodegradable polyesters such as $\varepsilon$-caprolactone and L-lactide was investigated as a function of temperature. MPEG-PCL was prepared by ring opening polymerization of $\varepsilon$-caprolactone in the presence of HClㆍEt$_2$O as monomer activator at room temperature. Also, MPEG-PLLA was prepared by ring opening polymerization of L-lactide in the presence of stannous octoate at 115$^{\circ}C$. The properties of block copolymers were investigated by $^1$H-NMR, IR, and GPC as well as the observation of thermo sensitive phase transition in aqueous solution. As the hydrophobic block length increased, the sol to gel transition temperature increased and curve of that steepen to lower concentration. To confirm the gel formation at body temperature, we observed the formation of gel in the mice body after injection of 20 wt% aqueous solution of each block copolymer. After surging, we investigated the gelation in mice. The results obtained in this study confirmed the feasibility as biomaterials of injectable implantation for controlled release of drug and protein delivery.

Introduction of Heterocycles at the 2-Position of Indoline as Ester Bioisosteres

  • Lee, Sung-Kyung;Yi, Kyu-Yang;Yoo, Sung-Eun
    • Bulletin of the Korean Chemical Society
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    • v.25 no.2
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    • pp.207-212
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    • 2004
  • In this study, we attempted to prepare compounds with heterocyclic replacements for metabolically unstable esters of benzopyranyl indole-2-carboxylic esters, which showed good in vitro and in vivo cardioprotective efficacies possibly through the opening of mitochondrial ATP-sensitive potassium channel ($K_{ATP}$). Initially, we tried to construct indolin-2-yl-heterocycles using unprotected indoline-2-carboxylic acid, but the cyclization was proceeded with oxidation of the indoline ring to the indole, which didn't react with benzopyranyl epoxide. Thus we introduced N-Boc group to deplete the electron density of the indoline ring. We successfully prepared various indolin-2-yl-heterocycles by the cyclization of the building blocks including carboxamide, ${\beta}$-hydroxy amide, hydrazide, nitrile starting from N-Boc-indoline-2-carboxylic acid.

A Development of Measurement System for Diathesis-Diagnosis (체질 진단을 위한 센서 시스템의 개발)

  • Jung, Yong-Rae;Kim, Seong-Woo
    • Proceedings of the KIEE Conference
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    • 2001.11c
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    • pp.260-263
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    • 2001
  • This paper is to develop the sensing system for opening-force measurement such as O-Ring muscular meridian. We designed to overcome the functional limit that the conventional force-sensor can measure just the closing-force. Therefore, the new sensor can meet a variety of application as well as O-Ring test. The structure of the new sensor is an actuator-type system using an electromagnet. That is made up of mechanical system, electromagnet, current transformer and computer interface circuit. Driving software and user interface program of the new sensor system also is explained in this paper.

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Thermal Shock Resistance of $Al_{2}O_{3}$- and Fe-$Al_{2}TiO_{5}$-based Castable Refractories

  • Liu, T.;Latella, B.A.;Bendeich, P.
    • The Korean Journal of Ceramics
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    • v.4 no.4
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    • pp.345-351
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    • 1998
  • Thermal shock resistance of $Al_2O_3$- and Fe-$Al_2TiO_5$-based Castable Refractories was studied using a central heating technique. Ring type specimens, 10mm thick and 20 and 100mm inner and outer diameters, respectively, were rapidly heated on the internal surface of the centre hole using a high power electrical heating element. The temperature field was measured experimentally and modelled using finite element analysis (FEA). The thermal stress field was also modelled using FEA. A radial notch was introduced to the ring specimens to enable calculation of the thermal stress intensity factors (SIF). A special LVDT device was incorporated in the thermal shock tester to monitor crack mouth opening displacement (COD). The thermal shock fracture initiation and crack propagation behaviour of the castable refractories were ascertained using the COD measurements and the fracture mechanics analysis data.

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