• Title/Summary/Keyword: 3-hydroxy-4-methylthiopyrrolidine

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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 and Antimicrobial Activity of 7-[(3-Methylthio or 3-Methylthiomethyl)pyrrolidinyl] quinolone-3-carboxylic Acid (7-[(3-메틸티오 또는 3-메틸티오메틸)피롤리디닐]퀴놀론-3-카르복실산의 합성과 항균작용)

  • Lee, Jae-Wook;Kang, Tae-Choong;Lee, Kyu-Sam;Son, Ho-Jung;Yoon, Geal-Joong;Yu, Young-Hyo;Kim, Dae-Young
    • YAKHAK HOEJI
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    • v.38 no.2
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    • pp.197-201
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    • 1994
  • A number of 7-[(3-methylthio or methylthiomethyl)pyrrolidiny]qui nolone-3-carboxylic acids were synthesized by condensation of 7-fluoro substituted quinolone-3-carboxylic acid with 3-methylthiopyrrolidine or 3-methylthiomet hylpyrrolidne. 3-Methylthiopyrrolidine or 3-methylthio-methylpyrrolidine which was prepared from N-benzyl-3-hydroxy pyrrolidine or 3-hydroxymethylpyrrolidine. 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-6,8-difluoro-7-(3-methylthiomethy-lpyrrolidinyl)-1,4-d ihydro-4-oxo-3-quinolinecarboxylic acid(7d) and 1-cyclopropyl-6- fluoro-8-chloro-7-(3-methylthiomethyl pyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (7f) showed the most potent in vitro antibacterial activity.

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