2,8,10-Trimethyl-1H,9H-pyrido[3,2-g]quinoline-4,6-dione | 182410-19-1

• 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: 2,8,10-Trimethyl-1H,9H-pyrido[3,2-g]quinoline-4,6-dione
• 英文别名: 2,8,10-Trimethylpyrido[3,2-g]quinoline-4,6(1H,9H)-dione；2,8,10-trimethyl-1,9-dihydropyrido[3,2-g]quinoline-4,6-dione
• CAS: 182410-19-1
• 化学式: C₁₅H₁₄N₂O₂
• 分子量: 254.288
• InChiKey: QIKWQLGORXJYPU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2,8,10-Trimethyl-1H,9H-pyrido[3,2-g]quinoline-4,6-dione 在 吡啶 、 tetraphosphorus decasulfide 作用下， 反应 4.0h， 生成 2,8,10-Trimethyl-1,9-dihydropyrido[3,2-g]quinoline-4,6-dithione
  参考文献：
  名称：

  New Pyridoquinoline Derivatives as Potential Inhibitors of the Fluoroquinolone Efflux Pump in Resistant Enterobacter aerogenes Strains

  摘要：

  Enterobacter aerogenes, one of the most frequently isolated nosocomial pathogens in France, is exhibiting increasing multidrug resistance mechanisms associated with a change in membrane permeability. For drugs of the quinolone family, mutations in the target and active efflux play a prominent role in the resistance. We report here the effect of several pyridoquinoline derivatives that restore a noticeable fluoroquinolone accumulation to resistant strains that overexpress the MarA activator. Studies of the energy-dependent quinolone efflux indicate that the most efficient derivatives tested probably inhibit the resistance process by acting as substrate competitors on the pump extruding intracellular norfloxacin.

  DOI：

  10.1021/jm010911z
• 作为产物：
  描述：

  2,6-二氨基甲苯 在 copper(II) sulfate 作用下， 以 二苯醚 、 乙醇 为溶剂， 反应 4.75h， 生成 2,8,10-Trimethyl-1H,9H-pyrido[3,2-g]quinoline-4,6-dione
  参考文献：
  名称：

  New Pyridoquinoline Derivatives as Potential Inhibitors of the Fluoroquinolone Efflux Pump in Resistant Enterobacter aerogenes Strains

  摘要：

  Enterobacter aerogenes, one of the most frequently isolated nosocomial pathogens in France, is exhibiting increasing multidrug resistance mechanisms associated with a change in membrane permeability. For drugs of the quinolone family, mutations in the target and active efflux play a prominent role in the resistance. We report here the effect of several pyridoquinoline derivatives that restore a noticeable fluoroquinolone accumulation to resistant strains that overexpress the MarA activator. Studies of the energy-dependent quinolone efflux indicate that the most efficient derivatives tested probably inhibit the resistance process by acting as substrate competitors on the pump extruding intracellular norfloxacin.

  DOI：

  10.1021/jm010911z

文献信息

• Synthesis of aza mono, bi and tricyclic compounds. Evaluation of their anti MDR activity
  作者：S Gallo

  DOI：10.1016/s0223-5234(02)01422-8

  日期：2003.1

  Anti MDR activity of a series of acridine, pyridoquinoline, quinoline and pyridine analogous amines was evaluated. Interesting activity is displayed by tricyclic compounds. Besides ring size, influence of the side chain was studied. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
• Synthesis and Antimalarial Activity of New 4,6-Dialkoxy- and 4,6-Bis(alkylthio)pyrido[3,2-g]quinoline Derivatives
  作者：Jacques Barbe、Carole Matias、Abdallah Mahamoud、Bruno Pradines、Jean-Claude Doury

  DOI：10.3987/com-96-7443

  日期：——
• New Pyridoquinoline Derivatives as Potential Inhibitors of the Fluoroquinolone Efflux Pump in Resistant <i>Enterobacter </i><i>a</i><i>erogenes </i>Strains
  作者：Jacqueline Chevalier、Siham Atifi、Annie Eyraud、Abdallah Mahamoud、Jacques Barbe、Jean-Marie Pagès

  DOI：10.1021/jm010911z

  日期：2001.11.1

  Enterobacter aerogenes, one of the most frequently isolated nosocomial pathogens in France, is exhibiting increasing multidrug resistance mechanisms associated with a change in membrane permeability. For drugs of the quinolone family, mutations in the target and active efflux play a prominent role in the resistance. We report here the effect of several pyridoquinoline derivatives that restore a noticeable fluoroquinolone accumulation to resistant strains that overexpress the MarA activator. Studies of the energy-dependent quinolone efflux indicate that the most efficient derivatives tested probably inhibit the resistance process by acting as substrate competitors on the pump extruding intracellular norfloxacin.