N-[(3,5-difluorophenyl)methyl]-5,8-dihydroxytetralin-2-carboxamide | 1621321-72-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-[(3,5-difluorophenyl)methyl]-5,8-dihydroxytetralin-2-carboxamide
• 英文别名: N-[(3,5-difluorophenyl)methyl]-5,8-dihydroxy-tetralin-2-carboxamide；N-[(3,5-difluorophenyl)methyl]-5,8-dihydroxy-1,2,3,4-tetrahydronaphthalene-2-carboxamide
• CAS: 1621321-72-9
• 化学式: C₁₈H₁₇F₂NO₃
• 分子量: 333.335
• InChiKey: KMEHUFPJEOFWDR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  69.6
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  5,8-dimethoxytetralin-2-carboxylic acid 在 三溴化硼 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 36.0h， 生成 N-[(3,5-difluorophenyl)methyl]-5,8-dihydroxytetralin-2-carboxamide
  参考文献：
  名称：

  Composition for treatment of pathogens that are resistant to tetracyclines

  摘要：

  该发明涉及与四环素结合在一起用于治疗由革兰氏阳性和革兰氏阴性病原体引起的细菌感染的化合物和药物组合物，对四环素耐药菌株尤为有效。这些化合物特异性地结合到TetR，从而阻止tet耐药基因的转录激活。这些化合物对四环素家族成员的活性具有增强作用，尤其对四环素、米诺环素、多西环素和替加环素在治疗四环素敏感、中间和四环素耐药病原体方面具有增强作用。

  公开号：

  EP2762134A1

文献信息

• [EN] COMPOSITION FOR TREATMENT OF PATHOGENS THAT ARE RESISTANT TO TETRACYCLINES<br/>[FR] COMPOSITION POUR LE TRAITEMENT DE PATHOGÈNES QUI SONT RÉSISTANTS AUX TÉTRACYCLINES
  申请人：BIOVERSYS AG

  公开号：WO2014118361A1

  公开（公告）日：2014-08-07

  The invention relates to compounds and pharmaceutical compositions useful in combination with tetracyclines in the treatment of bacterial infections caused by Gram- positive and Gram-negative pathogens, with particular efficacy in tetracycline resistant strains. These compounds specifically bind to TetR and therefore prevent the transcriptional activation of tet resistance genes. The compounds have a potentiating effect on the activity of members of the tetracycline family, in particular of tetracycline, minocycline, doxycycline and tigecycline, in the treatment of tetracycline susceptible, intermediate and tetracycline resistant pathogens.

  该发明涉及与四环素联合使用的化合物和药物组合物，用于治疗由革兰氏阳性和革兰氏阴性病原体引起的细菌感染，特别在四环素耐药菌株中具有显著疗效。这些化合物特异性地结合到TetR，从而阻止tet耐药基因的转录激活。这些化合物对四环素家族成员（特别是四环素、米诺环素、多西环素和替吉环素）的活性具有增强作用，在治疗四环素敏感、中间和四环素耐药病原体方面表现出效果。
• COMPOSITION FOR TREATMENT OF PATHOGENS THAT ARE RESISTANT TO TETRACYCLINES
  申请人：BIOVERSYS AG

  公开号：US20150359791A1

  公开（公告）日：2015-12-17

  The invention relates to compounds and pharmaceutical compositions useful in combination with tetracyclines in the treatment of bacterial infections caused by Gram-positive and Gram-negative pathogens, with particular efficacy in tetracycline resistant strains. These compounds specifically bind to TetR and therefore prevent the transcriptional activation of tet resistance genes. The compounds have a potentiating effect on the activity of members of the tetracycline family, in particular of tetracycline, minocycline, doxycycline and tigecycline, in the treatment of tetracycline susceptible, intermediate and tetracycline resistant pathogens.

  本发明涉及化合物和药物组合物，可用于与四环素联合治疗由革兰氏阳性和革兰氏阴性病原体引起的细菌感染，对四环素耐药菌株具有特殊疗效。这些化合物特异性结合TetR，从而防止tet耐药基因的转录激活。这些化合物对四环素家族成员的活性具有增强作用，特别是对四环素、米诺环素、多西环素和替加环素在四环素敏感、中间和四环素耐药病原体治疗中的活性具有增强作用。
• US9682079B2
  申请人：——

  公开号：US9682079B2

  公开（公告）日：2017-06-20
• Composition for treatment of pathogens that are resistant to tetracyclines
  申请人：Bioversys AG

  公开号：EP2762134A1

  公开（公告）日：2014-08-06

  The invention relates to compounds and pharmaceutical compositions useful in combination with tetracyclines in the treatment of bacterial infections caused by Gram-positive and Gram-negative pathogens, with particular efficacy in tetracycline resistant strains. These compounds specifically bind to TetR and therefore prevent the transcriptional activation of tet resistance genes. The compounds have a potentiating effect on the activity of members of the tetracycline family, in particular of tetracycline, minocycline, doxycycline and tigecycline, in the treatment of tetracycline susceptible, intermediate and tetracycline resistant pathogens.

  该发明涉及与四环素结合在一起用于治疗由革兰氏阳性和革兰氏阴性病原体引起的细菌感染的化合物和药物组合物，对四环素耐药菌株尤为有效。这些化合物特异性地结合到TetR，从而阻止tet耐药基因的转录激活。这些化合物对四环素家族成员的活性具有增强作用，尤其对四环素、米诺环素、多西环素和替加环素在治疗四环素敏感、中间和四环素耐药病原体方面具有增强作用。