1 0 0 0 IR dl-Cepharamineの合成研究
- 著者
- 瀬川 純 数野 憲二 松岡 正人 網本 功 尾崎 正邦 松田 真人 冨井 由文 北野 正彦 黄瀬 正博
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.43, no.7, pp.1238-1240, 1995-07-15 (Released:2008-03-31)
- 参考文献数
- 13
- 被引用文献数
- 3 7
Optically active isomers of 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1, 3]thiazeto[3, 2-a]quinoline-3-carboxylic acid (NM394, 3) were prepared through optical resolution of their racemic intermediate (±)-1 by high-performance liquid chromatography (HPLC). The absolute configuration at the C-1 position in the thiazetoquinolone ring of (-)-3 was confirmed by X-ray analysis of (-)-4 to be S. The in vitro antibacterial activity of (-)-3 was 2-8 times that of (+)-3.
- 著者
- 瀬川 純 数野 憲二 松岡 正人 白波瀬 一朗 尾崎 正邦 松田 真人 冨井 由文 北野 正彦 黄瀬 正博
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.43, no.1, pp.63-70, 1995-01-15 (Released:2008-03-31)
- 参考文献数
- 19
- 被引用文献数
- 6 13
A seried of 1, 8-disubstituted 6-fluoro-4-oxo-7-piperazinyl-4H-[1, 3]thiazeto[3, 2-a]quinoline-3-carboxylic acid derivatives was prepared and evaluated for antibacterial activity. In the 7-piperazinyl series, addition of a fluorine at C-8, which increased the in vitro activity for the 1-hydrogen and 1-methyl analogues and decreased it for the 1-phenyl analogue, improved the in vivo activity of all the analogues. Introduction of a methoxy group at C-8 of the 1-methyl-7-piperazinyl analogue also improved its in vivo antibacterial activity. The effect of 8-substituents on the in vitro and in vivo antibacterial activity of the 1-methyl-7-(4-methyl-1-piperazinyl) series is also discussed.
- 著者
- 瀬川 純 数野 憲二 松岡 正人 白波瀬 一朗 尾崎 正邦 松田 真人 冨井 由文 北野 正彦 黄瀬 正博
- 出版者
- 公益社団法人日本薬学会
- 雑誌
- Chemical & pharmaceutical bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.43, no.1, pp.63-70, 1995-01-15
A seried of 1,8-disubstituted 6-fluoro-4-oxo-7-piperazinyl-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives was prepared and evaluated for antibacterial activity. In the 7-piperazinyl series, addition of a fluorine at C-8,which increased the in vitro activity for the 1-hydrogen and 1-methyl analogues and decreased it for the 1-phenyl analogue, improved the in vivo activity of all the analogues. Introduction of a methoxy group at C-8 of the 1-methyl-7-piperazinyl analogue also improved its in vivo antibacterial activity. The effect of 8-substituents on the in vitro and in vivo antibacterial activity of the 1-methyl-7-(4-methyl-1-piperazinyl) series is also discussed.