(S)-N-[[3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl]methyl]-4-oxo-4-(4-thiomethyl)phenylbutanamide | 675609-11-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (S)-N-[[3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl]methyl]-4-oxo-4-(4-thiomethyl)phenylbutanamide
• 英文别名: N-[[(5S)-3-(3-fluoro-4-morpholino-phenyl)-2-oxo-oxazolidin-5-yl]methyl]-4-(4-methylsulfanylphenyl)-4-oxo-butanamide；N-[[(5S)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]-4-(4-methylsulfanylphenyl)-4-oxobutanamide
• CAS: 675609-11-7
• 化学式: C₂₅H₂₈FN₃O₅S
• 分子量: 501.579
• InChiKey: VSVADDCWTPQGJO-IBGZPJMESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  35
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  114
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  3-(4-甲基硫代苯甲酰基)丙酸 、 利奈唑胺碱 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 碳酸氢钠 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 24.25h， 以79%的产率得到(S)-N-[[3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl]methyl]-4-oxo-4-(4-thiomethyl)phenylbutanamide
  参考文献：
  名称：

  [EN] OXAZOLIDINONE DERIVATIVES, PROCESS FOR THEIR PREPERATION AND THEIR USE AS ANTIMYCOBACTERIAL AGENTS
  [FR] DERIVES D'OXAZOLIDINONE, LEUR PROCEDE DE PREPARATION ET LEUR UTILISATION COMME AGENTS ANTIMYCOBACTERIENTS

  摘要：

  新型化合物属于噁唑烷酮类，具有强效抗分枝杆菌特性，特别适用于治疗酸快速生长的微生物，如结核分枝杆菌、分枝杆菌内复合体、堪萨斯分枝杆菌和康萨分枝杆菌。该化合物及其药学上可接受的盐作为抗菌剂。还公开了一种抑制分枝杆菌细胞生长的方法，以及治疗结核分枝杆菌病、耐药性结核分枝杆菌、分枝杆菌内复合体、堪萨斯分枝杆菌和康萨分枝杆菌等分枝杆菌疾病的方法，包括给予所述化合物和/或其药学上可接受的盐的抗分枝杆菌有效量。还公开了一种制造所述化合物或其药学上可接受的盐的方法。

  公开号：

  WO2004026848A1

文献信息

• Novel antimycobacterial compounds
  申请人：Arora Kumar Sudershan

  公开号：US20050192275A1

  公开（公告）日：2005-09-01

  Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium -intracellular complex, M. fortuitum and M. kansai . The compound and its pharmaceutically acceptable salts thereof act as antibacterial agents. Also disclosed is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis , drug resistant Mycobacterium tuberculosis, Mycobacterium avium -intracellular complex, M. fortuitum and M. kansai , comprising administering an antimycobacterially effective amount of the said compound and/or pharmaceutically acceptable salts thereof. There is also disclosed a process for the manufacture of the said compound or its pharmaceutically acceptable salts.

  本发明涉及一类属于噁唑烷酮类的新化合物，具有强大的抗结核分枝杆菌的特性，尤其适用于治疗酸性快速生长的微生物，如结核分枝杆菌、肺巨细胞分枝杆菌、幸福分枝杆菌和关西分枝杆菌等。该化合物及其药用盐作为抗菌剂。本发明还公开了一种抑制分枝杆菌细胞生长的方法，以及一种治疗分枝杆菌感染的方法，如结核分枝杆菌、耐药结核分枝杆菌、肺巨细胞分枝杆菌、幸福分枝杆菌和关西分枝杆菌等，包括给予所述化合物和/或其药用盐的抗分枝杆菌有效量。本发明还公开了一种制备所述化合物或其药用盐的方法。
• Antimycobacterial compounds
  申请人：Lupin Limited

  公开号：US07691889B2

  公开（公告）日：2010-04-06

  Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.

  这是一种属于噁唑烷酮类的新化合物，具有强效的抗分枝杆菌特性，特别适用于治疗耐酸菌，如结核分枝杆菌、肺巨细胞分枝杆菌、堆积分枝杆菌、幸福分枝杆菌等。该化合物及其药学上可接受的盐具有抗菌作用。还提及了一种抑制分枝杆菌细胞生长的方法，以及一种治疗分枝杆菌病症的方法，如结核分枝杆菌、耐药性结核分枝杆菌、肺巨细胞分枝杆菌、堆积分枝杆菌、幸福分枝杆菌等，包括给予该化合物和/或药学上可接受的盐的抗分枝杆菌有效剂量。还提及了一种制备该化合物或其药学上可接受的盐的方法。
• [EN] OXAZOLIDINONE DERIVATIVES, PROCESS FOR THEIR PREPERATION AND THEIR USE AS ANTIMYCOBACTERIAL AGENTS<br/>[FR] DERIVES D'OXAZOLIDINONE, LEUR PROCEDE DE PREPARATION ET LEUR UTILISATION COMME AGENTS ANTIMYCOBACTERIENTS
  申请人：LUPIN LTD

  公开号：WO2004026848A1

  公开（公告）日：2004-04-01

  Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts thereof act as antibacterial agents. Also disclosed is a method for inhibiting growth of mycobacterial cells a well as a method of treating mycobacterial conditions such as Mycobacterium tuberculoses, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai, comprising administering an antimycobacterially effective amount of the said compound and/or pharmaceutically acceptable salts thereof. There is also disclosed a process for the manufacture of the said compound or its pharmaceutically acceptable salts.

  新型化合物属于噁唑烷酮类，具有强效抗分枝杆菌特性，特别适用于治疗酸快速生长的微生物，如结核分枝杆菌、分枝杆菌内复合体、堪萨斯分枝杆菌和康萨分枝杆菌。该化合物及其药学上可接受的盐作为抗菌剂。还公开了一种抑制分枝杆菌细胞生长的方法，以及治疗结核分枝杆菌病、耐药性结核分枝杆菌、分枝杆菌内复合体、堪萨斯分枝杆菌和康萨分枝杆菌等分枝杆菌疾病的方法，包括给予所述化合物和/或其药学上可接受的盐的抗分枝杆菌有效量。还公开了一种制造所述化合物或其药学上可接受的盐的方法。