最近のキノロン系抗菌剤の探索

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概要

• 論文の詳細を見る

• Nalidixic acid is a synthetic antibacterial agent active against Gram-negative organism. Since the introduction of Nalidixic acid in 1962, a large number of quinolone carboxylic acids have been synthesized. Early in the 1980s new agents such as norfloxacin, enoxacin, ofloxacin and ciprofloxacin, possessing the 6-fluoro substituent and the 7-piperazinyl group on the quinolone pharmacophore and collectively known as new quinolones or fluoroquinolones, were reported to have greatly improved potency and antibacterial spectra relative to old quinolones.<BR>Subsequently, considerable interest has been increasingly given to the structural manipulation of substituents on quinolone nucleus and detailed data for structure-activity relationships have been accumulated. This review will focus primarily on the recent advance in medicinal chemical studies of new quinolones in consideration of <I>in vitro</I> antibacterial activity, pharmacological properties, and physicochemical properties.

• 社団法人 有機合成化学協会の論文

著者

• 早川 勇夫

  第一製薬

• 木村 陽一

  Exploratory Laboratories I Daiichi Pharmaceutical Co. Ltd.

• 早川 勇夫

  第一製薬 (株) 探索第一研究所

• 竹村 真

  第一製薬 (株) 探索第一研究所

• 木村 陽一

  第一製薬 (株) 探索第一研究所

関連論文

• Synthesis of Antimicrobial Agents. VII. Synthesis and Antibacterial Activities of Furo [2,3-g] quinoline Derivatives
• Synthesis of Antimicrobial Agents. VI. Studies on the Synthesis of Furo [3,2-b] [1,8] naphthyridine Derivatives
• 最近のキノロン系抗菌剤の探索
• Synthesis and Structure-Activity Relationships of 7-[3-(1-Aminoalkyl)pyrrolidinyl]-and 7-[3-1-aminocycloalkyl)pyrrolidinyl]-quinolone Antibacterials
• Synthesis and Antibacterial Activities of Substituted 7-Oxo-2,3-dihydro-7H-pyrido [1,2,3-de] [1,4] benzoxazine-6-carboxylic Acids
• 最近のキノロン系抗菌剤の探索

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