Synthesis and Structure-Activity Relationships of 7-[3-(1-Aminoalkyl)pyrrolidinyl]-and 7-[3-1-aminocycloalkyl)pyrrolidinyl]-quinolone Antibacterials

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概要

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• A series of 7-[3-(1-aminoalkyl and 1-aminocycloalkyl)-1-pyrrolidinyl]quinolones have been prepared and their biological properties evaluated. Among them, 1-(S)-aminoalkyl derivatives exhibited potent antibacterial activities against gram-positive and gram-negative organisms. They had moderate lipophilicity and high aqueous solubility compared to their aminomethyl counterparts; e.g., the 3-(1-aminoethyl)-1-pyrrolidinyl compound (83) showed superior pharmacokinetic properties to its aminomethyl counterpart (6).

• 公益社団法人日本薬学会の論文
• 1994-07-15

著者

• 新子 省悟

  Exploratory Research Laboratories I, Daiichi Pharmaceutical Co., Ltd.,

• 新子 省悟

  Exploratory Research Laboratories I Daiichi Pharmaceutical Co. Ltd.

• 早川 勇夫

  Exploratory Laboratories I Daiichi Pharmaceutical Co. Ltd.

• 木村 陽一

  Exploratory Laboratories I, Daiichi Pharmaceutical Co., Ltd.,

• 高橋 雅宜

  Exploratory Laboratories I, Daiichi Pharmaceutical Co., Ltd.,

• 木村 陽一

  Exploratory Laboratories I Daiichi Pharmaceutical Co. Ltd.

• 高橋 雅宜

  Exploratory Laboratories I Daiichi Pharmaceutical Co. Ltd.

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• Synthesis and Structure-Activity Relationships of 7-[3-(1-Aminoalkyl)pyrrolidinyl]-and 7-[3-1-aminocycloalkyl)pyrrolidinyl]-quinolone Antibacterials
• 最近のキノロン系抗菌剤の探索

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