Synthesis and Antimicrobial Activity of 7-[(3-Methylthio or 3-Methylthiomethyl) -3-pyrrolinyl]quinolone-3-carboxylic Acids

7-[(3-메틸티오 또는 3-메틸티오메틸)-3-피롤리닐]퀴놀론-3-카르복실산의 합성과 항균작용

  • 이재욱 ((주)대웅제약 중앙연구소) ;
  • 손호정 ((주)대웅제약 중앙연구소) ;
  • 이규삼 ((주)대웅제약 중앙연구소) ;
  • 유영효 ((주)대웅제약 중앙연구소) ;
  • 김대영 (순천향대학교 화학과)
  • Published : 1994.10.30

Abstract

A number of 7-[(3-methylthio or methylthiomethyl)-3-pyrrolinyl] quinolone-3-carboxylic acids were synthesised by condensation of 7-fluoro substituted quinolone-3-carboxylic acid with 3-methylthio-3-pyrroline or 3-methylthiomethyl-3-pyrroline. 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 microoganisms. Among those 1-cyclopropyl-6,8-difluoro-7-[(3-methylthiomethyl) -3-pyrrolinyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12a) and 1-cycl opropyl-6-fluoro-8-chlore-7-[(3-methylthiomethyl)-3-pyrrolinly]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12b) showed the most potent in vitro antibacterial activity.

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