1,8-Naphthyridine-3-carboxylic acid, 7-[4-[4-[(5S)-5-[(acetylamino)methyl]-2-oxo-3-oxazolidinyl]-2-fluorophenyl]-1-piperazinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 1,8-Naphthyridine-3-carboxylic acid, 7-[4-[4-[(5S)-5-[(acetylamino)methyl]-2-oxo-3-oxazolidinyl]-2-fluorophenyl]-1-piperazinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-
• 英文别名: 7-[4-[4-[(5S)-5-(acetamidomethyl)-2-oxo-1,3-oxazolidin-3-yl]-2-fluorophenyl]piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
• 化学式: C₂₈H₂₈F₂N₆O₆
• 分子量: 582.564
• InChiKey: OHHWEUDPXJDZGT-SFHVURJKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  42
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  136
• 氢给体数：
  2
• 氢受体数：
  12

反应信息

• 作为产物：
  描述：

  环丙基萘啶羧酸 、 (S)-N-((3-(3-氟-4-(哌嗪-1-基)苯基)-2-氧代噁唑啉-5-基)甲基)乙酰胺 在 三甲基氯硅烷 作用下， 以 二甲基亚砜 为溶剂， 反应 10.0h， 以77%的产率得到1,8-Naphthyridine-3-carboxylic acid, 7-[4-[4-[(5S)-5-[(acetylamino)methyl]-2-oxo-3-oxazolidinyl]-2-fluorophenyl]-1-piperazinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-
  参考文献：
  名称：

  Design, Synthesis and Biological Evaluation of Oxazolidinone–Quinolone Hybrids

  摘要：

  Oxazolidinone-quinolone hybrids that combine the pharmacophores of a quinolone and an oxazolidinone were synthesised and shown to be active against a variety of resistant and susceptible Gram-positive and fastidious Gram-negative organisms. The best compounds in this series overcome all types of resistance in relevant clinical Gram-positive pathogens. The nature of the spacer greatly influences the antibacterial activity. The dual mode of action could be demonstrated for compounds having a piperazinyl spacer. Antibacterial activity was higher at acidic pH. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(03)00083-x

文献信息

• USE OF OXAZOLIDINONE-QUINOLINE HYBRID ANTIBIOTICS FOR THE TREATMENT OF ANTHRAX AND OTHER INFECTIONS
  申请人：Hubschwerlen Christian

  公开号：US20120322766A1

  公开（公告）日：2012-12-20

  The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.

  本发明涉及使用化合物，其中喹诺酮和噁唑烷酮的药效团经过稳定在生理条件下的连接剂化学连接在一起，用于治疗炭疽和其他感染病。
• Dual action antibiotics
  申请人：Hubschwerlen Christian

  公开号：US20050096343A1

  公开（公告）日：2005-05-05

  The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.

  本发明涉及式(I)化合物，其是有用的抗微生物剂，并且对多种多药耐药菌有效。
• Use of oxazolidinone-quinoline hybrid antibiotics for the treatment of anthrax and other infections
  申请人：Hubschwerlen Christian

  公开号：US20070155714A1

  公开（公告）日：2007-07-05

  The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.

  本发明涉及使用化合物，其中喹诺酮和噁唑烷酮的药效团通过在生理条件下稳定的链接剂进行化学连接，用于治疗炭疽病和其他感染。
• DUAL ACTION ANTIBIOTICS
  申请人：Hubschwerlen Christian

  公开号：US20110059946A1

  公开（公告）日：2011-03-10

  The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

  本发明涉及式（I）的化合物，它们是有用的抗微生物药物，并且对各种多药耐药细菌有效。
• Derivatives of oxazolidinones as antibacterial agents
  申请人：——

  公开号：US20040147545A1

  公开（公告）日：2004-07-29

  This invention discloses new fluorquinolonic derivatives of oxazolidinones of general formula (I) and processes for obtaining them, the corresponding pharmaceutical compositions and use thereof for manufacturing a medicament for the treatment of microbial infections. These new compounds are useful as antibacterial agents. Formula (I). Furthermore phenalen-type compounds according to general formula (II) are disclosed. Formula (II).

  本发明公开了通式(I)的噁唑烷酮的新氟喹诺酮衍生物、获得它们的工艺、相应的药物组合物及其用于制造治疗微生物感染的药物。这些新化合物可用作抗菌剂。式 (I)。此外，还公开了通式（II）的苯茚类化合物。式 (II).