5-Alkoxyimidazoquinolones as Potential Antibacterial Agents. Synthesis and Structure-Activity Relationships
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概要
- 論文の詳細を見る
4-Substituted 6-cyclopropyl-6,9-dihydro-5-methoxy-9-oxo-1H-imidazo[4,5-f]quinoline-8-carboxylic acids (6) and 8-substituted 1,5,6,11-tetrahydro-5-methyl-1-oxo-imidazo[4,5-g]pyrido[1,2,3-de][1,4]benzoxazine-2-carboxylic acids (7) were prepared as potential antibacterial quinolone derivatives. The appendages at C-4 of -6 and at C-8 of -7 were selected from 1-piperazinyl, 4-methylpiperazinyl, 3-aminopyrrolidinyl, and 3-aminomethylpyrrolidinyl groups. The 5-methoxyimidazoquinolones 6 were superior to the corresponding ofloxacin type analogues 7 in in vitro antibacterial activity. The activity of 6 was equipotent against S. aureus, but 2 to 16 times less potent against E. coli and P. aeruginosa compared to that of the 5-fluoro analogue 3.
- 社団法人日本薬学会の論文
- 1996-05-15
著者
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Matsumoto J
Discovery Research Laboratories Ii Dainippon Pharmaceutical Company Ltd.
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NAKANO Junji
Discovery Research Laboratories II, Dainippon Pharmaceutical Company, Ltd.,
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FUJITA Masahiro
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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EGAWA Hiroshi
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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MIYAMOTO Teruyuki
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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NAKANO Junji
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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MATSUMOTO Jun-ichi
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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Nakano J
Kaken Pharmaceutical Co. Ltd. Shizuoka Jpn
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Nakano Junji
Osaka Prefectural Senboku Nursery School
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Miyamoto Teruyuki
Exploratory Research Laboratories Dainippon Pharmaceutical Company Ltd.
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Fujita M
Vlsi Design And Education Center (vdec) The University Of Tokyo
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Egawa Hiroshi
Exploratory Research Laboratories Dainippon Pharmaceutical Company Ltd.
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