Synthetic Antibacterials. V. 7-Substituted 1-Ethyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acids

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概要

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• The reaction of nalidixic acid (1) with thionyl chloride afforded 1-ethyl-1,4-dihydro-4-oxo-7-trichloromethyl-1,8-naphthyridine-3-carboxylic acid (2) in high yield. Several 7-N-substituted carbamoyl-(3-47) and 7-(5-substituted benzimidazol-2-yl)-1-ethyl-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids (48-52) were prepared by treatment of 2 with appropriate amine and o-phenylenediamine, respectively. Alkaline treatment of 2 provided unexpected 7-hydroxy derivative (54), while the action of conc. sulfuric acid gave 3,7-dicarboxylic acids (53). The in vitro antibacterial activity and structural requirements of these compounds for broad spectrum activity were also discussed.

• 公益社団法人日本薬学会の論文
• 1975-12-25

著者

• 市場 みすず

  Pharmaceutical Institute, School of Medicine, Keio, University

• 千賀 慶太郎

  Pharmaceutical Institute, School of Medicine, Keio, University

• 千賀 慶太郎

  Pharmaceutical Institute School Of Medicine Keio University

• 千賀 慶太郎

  慶応大 病院

• 千賀 慶太郎

  慶応義塾大学病院薬剤部

• 西垣 貞男

  Pharmaceutical Institute, School of Medicine, Keio University

• 米田 文郎

  Pharmaceutical Sciences, Kumamoto University

• 篠村 和子

  Pharmaceutical Institute School Of Medicine Keio University

• 深沢 信乃夫

  Pharmaceutical Institute, School of Medicine, Keio University

• 金堀 猷子

  Pharmaceutical Institute, School of Medicine, Keio University

• 市場 みすず

  Pharmaceutical Institute School Of Medicine Keio University

• 西垣 貞男

  Pharmaceutical Institute School Of Medicine Keio University

• 西垣 貞雄

  Pharmaceutical Institute School Of Medicine Keio University

• 深沢 信乃夫

  Pharmaceutical Institute School Of Medicine Keio University

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