Imidazo- and Triazoloquinolones as Antibacterial Agents. Synthesis and Structure-Activity Relationships
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概要
- 論文の詳細を見る
4,5-Disubstituted 6-cyclopropyl-6,9-dihydro-9-oxo-1H-imidazo- (30-32) and triazolo[4,5-f]quinoline-8-carboxylic acids (33-35) were synthesized starting from 5,6-diaminoquinolones 25. The imidazoquinolones 30-32 were equal or superior to the corresponding triazoloquinolone analogues 33-35 in in vitro antibacterial activity. As for the C-5 substituents, a fluorine atom was the most favorable of the three groups, H, F, and Cl. Among the compounds prepared, 4-(cyclic amino)-5-fluoro-imidazoquinolones 31a-d showed potent and well-balanced antibacterial activity against both gram-positive and gram-negative bacteria. Structure-activity relationships for the C-4 substituents (cyclic amino groups) were also examined in detail.
- 公益社団法人日本薬学会の論文
- 1995-12-15
著者
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松本 純一
Exploratory Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
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松本 純一
Exploratory Research Laboratories Dainippon Pharmaceutical Company Ltd.
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松本 純一
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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藤田 昌宏
Exploratory Research Laboratories Dainippon Pharmaceutical Company Ltd.
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Miyamoto Tomofumi
Graduate School Of Pharmaceutical Sciences Kyushu Univ.
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江川 宏
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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片岡 昌宏
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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宮本 晧之
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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中野 純次
Exploratory Research Laboratories, Dainippon Pharmaceutical Company, Ltd.,
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江川 宏
Exploratory Research Laboratories Dainippon Pharmaceutical Company Ltd.
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中野 純次
Exploratory Research Laboratories Dainippon Pharmaceutical Company Ltd.
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中野 純次
大日本製薬株式会社総合研究所
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松本 純一
Exploratory Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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Maruta Tomoki
Graduate School Of Pharmaceutical Sciences Kyushu University
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片岡 昌宏
Nagasaki Univ. Nagasaki Jpn
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Fujita M
Univ. Tokyo
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