약학회지 (YAKHAK HOEJI)
- 제38권2호
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- Pages.197-201
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- 1994
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- 0377-9556(pISSN)
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- 2383-9457(eISSN)
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
- 이재욱 ((주)대웅제약 중앙연구소) ;
- 강태충 ((주)대웅제약 중앙연구소) ;
- 이규삼 ((주)대웅제약 중앙연구소) ;
- 손호정 ((주)대웅제약 중앙연구소) ;
- 윤길중 ((주)대웅제약 중앙연구소) ;
- 유영효 ((주)대웅제약 중앙연구소) ;
- 김대영 (순천향대학교 화학과)
- Lee, Jae-Wook (R&D Center, Dae Woong Pharmaceutical Co. Ltd.) ;
- Kang, Tae-Choong (R&D Center, Dae Woong Pharmaceutical Co. Ltd.) ;
- Lee, Kyu-Sam (R&D Center, Dae Woong Pharmaceutical Co. Ltd.) ;
- Son, Ho-Jung (R&D Center, Dae Woong Pharmaceutical Co. Ltd.) ;
- Yoon, Geal-Joong (R&D Center, Dae Woong Pharmaceutical Co. Ltd.) ;
- Yu, Young-Hyo (R&D Center, Dae Woong Pharmaceutical Co. Ltd.) ;
- Kim, Dae-Young (Department of Chemistry, Soonchunhyang University)
- 발행 : 1994.04.30
초록
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.
키워드