N'-hexylciprofloxacin

• 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: N'-hexylciprofloxacin
• 英文别名: 1-cyclopropyl-6-fluoro-7-(4-hexylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid；1-Cyclopropyl-6-fluoro-7-(4-hexylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
• 化学式: C₂₃H₃₀FN₃O₃
• 分子量: 415.508
• InChiKey: NMELGMVWAQXJBX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  30
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  64.1
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  溴己烷 、 环丙沙星 在 三乙胺 、 potassium iodide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 N'-hexylciprofloxacin
  参考文献：
  名称：

  Anionic fluoroquinolones as antibacterials against biofilm-producing Pseudomonas aeruginosa

  摘要：

  Pseudomonas aeruginosa is a common biofilm-forming bacterial pathogen implicated in diseases of the lungs. The extracellular polymeric substances (EPS) of respiratory Pseudomonas biofilms are largely comprised of anionic molecules such as rhamnolipids and alginate that promote a mucoid phenotype. In this Letter, we examine the ability of negatively-charged fluoroquinolones to transverse the EPS and inhibit the growth of mucoid P. aeruginosa. Anionic fluoroquinolones were further compared with standard antibiotics via a novel microdiffusion assay to evaluate drug penetration through pseudomonal alginate and respiratory mucus from a patient with cystic fibrosis. (C) 2016 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2016.01.012

文献信息

• Novel fluoroquinolones and use thereof to treat bacterial infections
  申请人：Université Paris 6 Pierre et Marie Curie UPMC

  公开号：EP2957561A1

  公开（公告）日：2015-12-23

  The present invention relates to novel fluoroquinolones possessing a piperazine moiety substituted by a long alkyl chain, pharmaceutical compositions or medicament containing them and use thereof to treat bacterial infection.

  本发明涉及一种新型氟喹诺酮，其带有由长烷基链取代的哌嗪基团，以及含有它们的药物组合物或药物，用于治疗细菌感染。
• Fluoroquinolones and use thereof to treat bacterial infections
  申请人：UNIVERSITÉ PIERRE ET MARIE CURIE—PARIS 6 (UPMC)

  公开号：US10087165B2

  公开（公告）日：2018-10-02

  The present invention relates to novel fluoroquinolones, pharmaceutical compositions or medicament containing them and use thereof to treat bacterial infection.

  本发明涉及新型氟喹诺酮类药物、药物组合物或含有它们的药物以及使用它们治疗细菌感染。
• NOVEL FLUOROQUINOLONES AND USE THEREOF TO TREAT BACTERIAL INFECTIONS
  申请人：Université Pierre et Marie Curie - Paris 6 (UPMC)

  公开号：EP3157911A1

  公开（公告）日：2017-04-26
• [EN] NOVEL FLUOROQUINOLONES AND USE THEREOF TO TREAT BACTERIAL INFECTIONS<br/>[FR] NOUVEAUX FLUOROQUINOLONES ET LEUR UTILISATION POUR TRAITER DES INFECTIONS BACTÉRIENNES
  申请人：UNIVERSITÉ PIERRE ET MARIE CURIE PARIS 6 UPMC

  公开号：WO2015193454A1

  公开（公告）日：2015-12-23

  The present invention relates to novel fluoroquinolones, pharmaceutical compositions or medicament containing them and use thereof to treat bacterial infection.
• Anionic fluoroquinolones as antibacterials against biofilm-producing Pseudomonas aeruginosa
  作者：Timothy E. Long、Lexie C. Keding、Demetria D. Lewis、Michael I. Anstead、T. Ryan Withers、Hongwei D. Yu

  DOI：10.1016/j.bmcl.2016.01.012

  日期：2016.2

  Pseudomonas aeruginosa is a common biofilm-forming bacterial pathogen implicated in diseases of the lungs. The extracellular polymeric substances (EPS) of respiratory Pseudomonas biofilms are largely comprised of anionic molecules such as rhamnolipids and alginate that promote a mucoid phenotype. In this Letter, we examine the ability of negatively-charged fluoroquinolones to transverse the EPS and inhibit the growth of mucoid P. aeruginosa. Anionic fluoroquinolones were further compared with standard antibiotics via a novel microdiffusion assay to evaluate drug penetration through pseudomonal alginate and respiratory mucus from a patient with cystic fibrosis. (C) 2016 Elsevier Ltd. All rights reserved.