Glycinyl-spermine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Glycinyl-spermine
• 英文别名: glycinoylspermine；glycylspermine；Glycyl spermine；2-amino-N-[3-[4-(3-aminopropylamino)butylamino]propyl]acetamide
• 化学式: C₁₂H₂₉N₅O
• 分子量: 259.395
• InChiKey: SQYYUNVPCWLGJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  18
• 可旋转键数：
  13
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  105
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  精胺 、 Fmoc-甘氨酸 生成 Glycinyl-spermine
  参考文献：
  名称：

  Novel spermine–Amino acid conjugates and basic tripeptides enhance cleavage of the hairpin ribozyme at low magnesium ion concentration

  摘要：

  Combinations of the polyamine spermine and magnesium ions synergize to dramatically enhance cleavage of the hairpin ribozyme. Certain synthetic basic tripeptides stimulate hairpin cleavage significantly at limiting magnesium ion concentration, notably the tripeptide Of L-diaminobutyric acid (Dab). Of a range of novel synthetic spermine-amino acid conjugates, L-Dabspermine (but not D-Dab nor other amino acid conjugates) was more effective than spermine itself. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00608-4

文献信息

• Polyamine analogues as therapeutic and diagnostic agents
  申请人：MediQuest Therapeutics, Inc.

  公开号：EP1867633A1

  公开（公告）日：2007-12-19

  Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

  本研究公开了新型多胺转运抑制剂，其抑制常数比已知化合物的抑制常数低两个数量级。这些多胺类似物是治疗需要抑制多胺转运或其他多胺结合蛋白的疾病（如癌症和血管成形术后损伤）的有用药物。公开了获得多胺类似物的新型化学合成方法，包括组合多胺库的生产。这些方法产生的类似物具有理想的活性，既可用于诊断和研究测定，也可用于治疗。本发明的检测方法可用于高通量筛选目标，以发现与多胺系统相互作用的药物。
• COMPOSITION FOR ORAL DELIVERY COMPRISING MGBG FOR USE IN TREATING MULTIPLE SCLEROSIS
  申请人：Pathologica LLC

  公开号：EP3473247A1

  公开（公告）日：2019-04-24

  The present invention relates to an oral pharmaceutical composition, comprising methylglyoxal bis(guanylhydrazone) (MGBG) together with at least one oral pharmaceutically acceptable excipient, for use in the treatment or delaying the onset or development of multiple sclerosis when orally administered to a subject.

  本发明涉及一种口服药物组合物，包括甲基乙二醛双（鸟苷腙）（MGBG）和至少一种口服药物可接受赋形剂，用于口服给受试者治疗或延缓多发性硬化症的发作或发展。
• MITOGUAZONE FOR PREVENTING THE RELAPSE OR THE PROGRESSION OF MULTIPLE SCLEROSIS
  申请人：Pathologica LLC

  公开号：EP3831372A1

  公开（公告）日：2021-06-09

  Disclosed herein are new oral pharmaceutical compositions of SAMDC inhibitors, polyamine analogs, and polyamine biosynthesis inhibitors, and their application for the treatment of conditions including demyelinating diseases, autoimmune disorders affecting the nervous system, and other neurodegenerative conditions.

  本文公开了SAMDC抑制剂、多胺类似物和多胺生物合成抑制剂的新型口服药物组合物，以及它们在治疗脱髓鞘疾病、影响神经系统的自身免疫性疾病和其他神经退行性疾病等疾病中的应用。
• Methods and compositions for treatment of demyelinating diseases
  申请人：Pathologica LLC

  公开号：US10350178B2

  公开（公告）日：2019-07-16

  Disclosed herein is a method of prevention of progression of a multiple sclerosis in a patient, comprising the administration of methylglyoxal bis(guanylhydrazone) (MGBG) to the patient in need thereof. Also disclosed herein is a method of prevention or reduction in severity of the initiation phase of autoimmune response in a patient having multiple sclerosis, comprising the administration of MGBG to the patient in need thereof.

  本文公开了一种预防多发性硬化症患者病情恶化的方法，包括向有需要的患者施用甲基乙二醛双（鸟苷酸腙）（MGBG）。本文还公开了一种预防多发性硬化症患者自身免疫反应起始阶段或减轻其严重程度的方法，包括对有需要的患者施用 MGBG。
• Novel compositions of TLR7 and/or TLR8 agonists conjugated to lipids
  申请人：Invivogen

  公开号：EP2674170B1

  公开（公告）日：2014-11-19