7-amino-6-nitro-4-oxo-1H-quinoline-3-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 7-amino-6-nitro-4-oxo-1H-quinoline-3-carboxylic acid
• 化学式: C₁₀H₇N₃O₅
• 分子量: 249.183
• InChiKey: BGNXNZBYTULONX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  138
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-氯-4-氟-5-硝基苯甲酰氯 在 硫酸 、 乙酸酐 、 三乙胺 、 magnesium chloride 作用下， 以 溶剂黄146 、 乙腈 为溶剂， 反应 6.0h， 生成 7-amino-6-nitro-4-oxo-1H-quinoline-3-carboxylic acid
  参考文献：
  名称：

  New 6-nitroquinolones: synthesis and antimicrobial activities

  摘要：

  Pursuing our searches on quinolonecarboxylic acids we used a simple three-step one pot procedure to synthesize novel 1,7-disubstituted-6-nitroquinolones. The new derivatives were tested against Mycobacterium tuberculosis and Mycobacterium avium complex (MAC) as well as against both gram-positive and gram-negative bacteria. In vitro assays showed some derivatives were endowed with good inhibiting activities against tested mycobacteria. Some derivatives were also found more potent than ciprofloxacin and ofloxacin (used as reference drugs) against gram-positive bacteria.

  DOI：

  10.1016/j.farmac.2004.01.014

文献信息

• New 6-nitroquinolones: synthesis and antimicrobial activities
  作者：Gianluca Sbardella、Antonello Mai、Marino Artico、Maria Giovanna Setzu、Graziella Poni、Paolo La Colla

  DOI：10.1016/j.farmac.2004.01.014

  日期：2004.6

  Pursuing our searches on quinolonecarboxylic acids we used a simple three-step one pot procedure to synthesize novel 1,7-disubstituted-6-nitroquinolones. The new derivatives were tested against Mycobacterium tuberculosis and Mycobacterium avium complex (MAC) as well as against both gram-positive and gram-negative bacteria. In vitro assays showed some derivatives were endowed with good inhibiting activities against tested mycobacteria. Some derivatives were also found more potent than ciprofloxacin and ofloxacin (used as reference drugs) against gram-positive bacteria.