Synthesis and Antibacterial Activity of Novel Pyridobenzoxazine Analogues
スポンサーリンク
概要
- 論文の詳細を見る
A series of novel LVFX (7) analogues bearing 4,4-dialkyl-3-aminopyrrolidines at the C-10 position of pyridobenzoxazine was synthesized and their antibacterial activities, pharmacokinetics and acute toxicities in animals were evaluated. Non-alkylated pyrrolidine derivative 26a showed greater activity than LVFX (7) against gram-positive and gram-negative bacteria including Pseudomonas aeruginosa, but 26a possessed high acute toxicity in mice and unfavorable pharmacokinetics in rats. When compared with 26a, 4,4-dialkylated derivatives 26c, e, g showed more potent activity against gram-positive bacteria along with an improvement of pharmacokinetics and reduction of acute toxicity. Increases in lipophilicity by alkylation on the pyrrolidine ring resulted in a good influence on the above profiles.
- 公益社団法人日本薬学会の論文
- 1998-11-15
著者
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Takemura M
Life Science Research Center Mie University
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Hayakawa I
New Product Research Laboratories I Daiichi Pharmaceutical Co. Ltd.
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KAWAKAMI Katsuhiro
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd.,
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ATARASHI Shohgo
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd.,
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KIMURA Youichi
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd.,
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TAKEUMURA Makoto
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd.,
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HAYAKAWA Isao
New Product Research Laboratories I, Daiichi Pharmaceutical Co., Ltd.,
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Atarashi S
New Product Research Laboratories I Daiichi Pharmaceutical Co. Ltd.
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Kimura Youichi
New Product Research Laboratories I Daiichi Pharmaceutical Co. Ltd.
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Kawakami K
Daiichi Pharmaceutical Co. Ltd. Tokyo Jpn
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Kawakami Katsuhiro
New Product Research Laboratories I Daiichi Pharmaceutical Co. Ltd.
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