(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10,13-tetrahydroxy-11-[(2S,3R,6R)-3-hydroxy-6-methyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one | 688002-52-0

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酯类和类似物
• 英文名称: (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10,13-tetrahydroxy-11-[(2S,3R,6R)-3-hydroxy-6-methyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one
• CAS: 688002-52-0
• 化学式: C₂₈H₅₃NO₉
• 分子量: 547.73
• InChiKey: MQRQPCFMHXKODQ-YTYMPLCASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  38
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.96
• 拓扑面积：
  149
• 氢给体数：
  5
• 氢受体数：
  10

文献信息

• Azithromycin derivatives with epithelial barrier enhancement properties
  申请人：EpiEndo Pharmaceuticals ehf

  公开号：US10723752B2

  公开（公告）日：2020-07-28

  The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.

  本发明提供了新型化合物，它们是阿奇霉素的衍生物，本发明人发现它们具有较低的抗菌活性，但具有显著的上皮屏障增强特性。本发明进一步提供了这些化合物作为药物的用途，特别是用于治疗或预防由上皮细胞或组织缺陷引起的疾病或病症，或受益于上皮屏障功能增强或恢复的疾病或病症，例如呼吸道疾病。
• Compounds
  申请人：EpiEndo Pharmaceuticals ehf

  公开号：US20220106349A1

  公开（公告）日：2022-04-07

  The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.