Synthesis of Possible Metabolites of 1-Cyclopropyl-1,4-dihydro-6-fluoro-5-methyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic Acid (Grepafloxacin, OPC-17116)

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概要

• 論文の詳細を見る

• Grepafloxacin (1-cyclopropyl-1,4-dihydro-6-fluoro-5-methyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinoline-carboxylic acid, OPC-17116) (1) exhibits potent and broad-spectrum in vitro and in vivo antibacterial activity. In order to identify the structures of the metabolites of grepafloxacin, 17 possible metabolites were prepared. Among them, 6 compounds were found to be actual metabolites (2a, b, 4a, b and 6a, b) of grepafloxacin in rats, dogs and/or humans. The antibacterial activities of these metabolites were found to be weaker than that of grepafloxacin.

• 公益社団法人日本薬学会の論文
• 1995-12-15

著者

• 大森 和則

  大塚製薬株式会社微生物研究所

• 大黒 絹枝

  大塚製薬株式会社微生物研究所

• 松原 淳

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 内多 稔

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 森田 清司

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 大坪 健児

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 大谷 直明

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• Morita S

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Uchida Masaki

  Faculty Of Pharmaceutical Sciences Josai University

• 大谷 直明

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 川野 芳和

  Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 大森 和則

  Microbiological Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• 大黒 絹枝

  Microbiological Research Institute, Otsuka Pharmaceutical Co., Ltd.,

• Uchida Masaatsu

  Departments Of Pharmacology Meiji Pharmaceutical University

• Uchida Mihoko

  Department Of Biochemistry Faculty Of Pharmaceutical Sciences Hoshi University

• Morita S

  Kagawa Medical Univ. Kagawa Jpn

• Uchida M

  Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn

• Morita Shushi

  Department Of Hospital Pharmacy Kagawa University

• 大坪 健児

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• 森田 清司

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Ohtani T

  Minase Research Institute Ono Pharmaceutical Co. Ltd.

• 川野 芳和

  Tokushima Research Institute Otsuka Pharmaceutical Co. Ltd.

• Ohmori K

  Tokyo Univ. Pharmacy And Life Sci. Tokyo Jpn

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