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

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

A number of 7-[(3-methylthio or methylthiomethyl)pyrrolidinyl]quinolone-3-carboxylic acids were synthesized by condensation of 7-fluoro substituted quinolone-3-carboxylic acid with 3-methylthiopyrrolidine or 3-methylthiomethylpyrrolidine. 3-Methylthiopyrrolidine or 3-methylthiomethylpyrrolidine 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 microoranisms. Among those 1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethy- lpyrrolidinyl)-1,4-dihydro-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.