Synthesis and Antibacterial Activities of Optically Active Substituted 1,2-Dihydro-6-oxo-6H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic Acids
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概要
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A series of optically active substituted 1,2-dihydro-6-oxo-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids was prepared via optically active 2-methyl-4,5-difluoroindoline (10) and tested for antibacterial activities. Among them, (2S)-9-[(3R, 1'S)-3-(1'-amino)ethyl-1-pyrrolidinyl]-8-fluoro-1,2-dihydro-2-methyl-6-oxo-6H-pyrrolo[3,2,1,-ij]-quinoline-5-carboxylic acid (19) showed potent activity against gram-positive bacteria and (2S)-8-fluoro-1,2-dihydro-2-methyl-9-(3-methyl-1-piperazinyl)-6-oxo-6H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acid (16) exhibited well balanced in vitro activity, good intravenous efficacy, and high aqueous solubility.
- 社団法人日本薬学会の論文
- 1995-10-15
著者
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辻 浩一
Microbiological Research Institute Otsuka Pharmaceutical Co. Ltd.
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石川 廣
Microbiological Research Institute Otsuka Pharmaceutical Co. Ltd.
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壺内 英継
Microbiological Research Institute, Otsuka Pharmaceutical Co., Ltd.,
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壺内 英継
Microbiological Research Institute Otsuka Pharmaceutical Co. Ltd.
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Tsuji K
School Of Pharmaceutical Science University Of Shizuoka
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