• Title/Summary/Keyword: LTD4

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Synthesis and Antimicrobial Activity of 7-[3-Hydroxy-(4-methylthio or 4-methylthiomethyl)pyrrolidinyl]quinoline-3-carboxylic Acids (7-[3-히드록시-(4-메틸티오 또는 4-메틸티오메틸)피롤리디닐]퀴놀린-3-카르복실산의 합성과 항균작용)

  • Lee, Jae-Wook;Son, Ho-Jung;Lee, Kyu-Sam;Yu, Young-Hyo;Yoon, Geal-Jung
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.677-682
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    • 1994
  • A number of 7-[3-hydroxy-(4-methylthio or 3-methylthiomethyl)pyrrolidinyl]quinoline-3-carboxylic acids were synthesized by condensation of 7-fluoro substituted quinoline-3-carboxylic acid with 3-hydroxy-4-methylthiopyrrolidine or 3-hydroxy-4-methylthiomethylpyrrolidine. The in vitro antimicrobial activity of them were tested against twenty species of Gram-positive or Gram-negative microorganisms. It showed remarkable antibacterial activity, particularly against Gram-positive microorganisms. Among those 1-cyclopropyl-5-amino-6,8-difluoro 7-(3-hydroxy-4-methylthiomethylpyrrolidinyl)-1,4-dihyd ro-4-oxo-3-quinolinecarboxylic acid(12d) and 1-cyclopropyl-6-fluoro-8-methoxy-7-(3-hydroxy-4-methylthiometby1pyrrolinyl)-1,4-dihydro-4-oxo-3-quinolinocarboxylic acid(12g) showed the most potent in vitro antibacterial activity, and 12d showed better antibacterial activity against MRSA compared to ciprofloxacin and sparfloxacin.

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Synthesis of UV-Curable Modified (3,4-epoxycyclohexane)methyl 3,4-epoxycyclohexylcarboxylate Acrylate (자외선 경화형 변성 (3,4-epoxycyclohexane)methyl 3,4-epoxycyclohexylcarboxylate 아크릴레이트의 합성)

  • Lee, Jongmin;Yi, Hwanpyo;Lee, Sanggun;Park, Hyungnam;Choi, Kangsik;Kim, Dojin
    • Korean Journal of Materials Research
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    • v.27 no.4
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    • pp.199-205
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    • 2017
  • In this study, (3,4-epoxycyclohexane)methyl 3,4-epoxycyclohexylcarboxylate acrylate was synthesized by reacting (3,4-epoxycyclohexane)methyl 3,4-epoxycyclohexylcarboxylate with acrylic acid to minimize hardening shrinkage and to improve heat resistance, which are known as disadvantages of photopolymers for 3D printing application. Urethane acrylate was synthesized by reacting 1,3,5-triazine-2,4,6-triamino alcohol, 2-hexylethyl acrylate, and isophorone diisocyanate in order to improve the mechanical properties without deteriorating the heat resistance. The physical properties before and after the synthesis of the acrylate and the mechanical properties when the urethane acrylate was applied were investigated. The reaction progress of the composite was examined by FTIR and $^{13}C$ NMR. The heat deflection temperature, flexural strength, and surface hardness of the molding were measured. The curing behavior by Photo-DSC ultraviolet irradiation was also examined.

Development of the 4kw photovoltaic inverter for using in Japan (일본형 4kW 태양광 PCU 개발)

  • Kim, Ho-Yeol;Yun, Dong-Jin;Yun, Sun-Jae;Kim, Young-Min;Kim, Hee-Jung;Park, Tae-Bum
    • Proceedings of the KIEE Conference
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    • 2015.07a
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    • pp.1072-1073
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    • 2015
  • 현재 일본에서는 6kW이하의 태양광 인버터는 다수대 연계 대응형 태양광 발전 시스템 계통연계 보호 장치의 개별 시험방법을 만족하도록 하고 있다. 이 규격은 기존 인증보다 강화된 규격으로 자사에서는 기존 인증을 취득한 개발한 역량을 바탕으로 이 규격을 만족할 수 있는 4kW급 태양광 인버터를 개발하는 중이다.

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Lifetime improvement of 4P Magnetic Contactor (4P 전자접촉기의 수명 향상)

  • Lee, Kyung-Ku;Ryu, Jong-Sang;Kim, Gyeon-Mook;Park, Ji-Hong;Jo, Hyun-Kil;Seo, Jung-Min
    • Proceedings of the KIEE Conference
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    • 2001.10a
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    • pp.42-44
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    • 2001
  • This paper proposes impact vibration theory of magnetic contactor moving mechanism and correlation test the bouncing time with the spring load. Mechanical and electrical lifetime is under the influence of impact vibration of magnetic contactor moving mechanism. In shortage of technique, we have experienced many difficulties in magnetic contactor development. By this research, we analyzed total moving mechanism and applied results to optimum 4p magnetic contactor development.

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Comparison of CYP 3A4 metabolism between DA-8159 and Sildenafil in vitro and in vivo

  • Park, Kyung-Jin;Youn, Hae-Sun;Shim, Hyun-Joo;Kim, Soon-Hoe;Yoo, Moo-Hi;Kim, Won-Bae
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.253.1-253.1
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    • 2002
  • DA-8159 is a new PDEV inhibitor, synthesized by Dong-A Pharm, as an oral agent to treat male erectile dysfunction. DA-8159 and sildenafil are mainly metabolized by cytochrome P450 enzyme CYP 3A4. In this study. we compared the metabolism of DA-8159 with sildenafil in vitro and in vivo. First, we quantified the remaining gatio of original compound, DA-8159 and sidenafil., after we incubated drugs for 30 minutes with human liver microsome cytochrome P 450 3A4. (omitted)

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Synthesis and Biological Evaluation of 4-Phenyl-1-(indoline-5-sulfonyl)-2-imidazolone Derivatives as Potential Antitumor Agents

  • Park, Dongrak;Lee, Jungah;Hyunsook Hwang;Lee, Dugkeun;Sungjune Yoon;Yongho Chung;Sanghun Jung;Lee, Moonsun
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.73-73
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    • 1997
  • A series of 4-phenyl-1-(indoline-5-sulfonyl)-2-imidazolone derivatives has been synthesized starting from 2-bromoacetophenone. Reaction of 2-aminoacetophenone obtained from 2-bromoacetophenon by Delepin synthesis and potassium cyanate affords 1,3-dihydro-4-phenyl-2-imidazolone. This key intermediate was treated with sodium hydride and N-trifluoroacetyl-indoline-5-sulfonylchloride, and trifluoroacetyl group was deprotected to give 4-Phenyl-1-(indoline-5-sulfonyl)-2-imidazolone. Various substituents were introduced on the nitrogen of indoline. Antitumor activity of this series of compound was evaluated by MTT method. Nearly all of the compounds showed broad-spectrum activity.

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Synthesis and SAR Studies for the Inhibition of TNF-$\alpha$ Production. Part 2. 2-[3-(Cyclopenthloxy)4-Methoxyphenyl]-Substituted-1-Isoindolinone Derivatives

  • Park, Joon-Seok;Moon, Seong-Cheol;Baik, Kyung-Up;Cho, Jae-Youl;Yoo, Eun-Sook;Byun, Young-Seok;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • v.25 no.2
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    • pp.137-142
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    • 2002
  • This study describes the synthesis and in vitro evaluation of 2-[3- (Cyclopenthloxy) 4-Methoxyphenyl] - Substituted-1-Isoindolinone derivatives substituted on benzene moiety of isoindoline ring for the inhibition of $TNF-{\alpha}$ production. From this study, we have found the 6-C position on isoindolinone ring is an optimal derivatization site. Among the compounds synthesized, 6-ammo-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (6) was the most potent in inhibitory activity of $TNF-{\alpha}$ production in LPS-stimulated RAW264.7 cells.