1,16-diamino-4,8,13-triazahexadecane

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1,16-diamino-4,8,13-triazahexadecane
• 英文别名: N-(3-aminopropyl)-N'-[3-(3-aminopropylamino)propyl]butane-1,4-diamine
• 化学式: C₁₃H₃₃N₅
• 分子量: 259.439
• InChiKey: RXOMMWRZPQYBPT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  18
• 可旋转键数：
  15
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  88.1
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  (N¹,N⁴,N⁹,N¹³-tetra-tert-butoxycarbonyl)-1,16-diamino-4,9,13-triazahexadecane 在 三氟乙酸 作用下， 生成 1,16-diamino-4,8,13-triazahexadecane
  参考文献：
  名称：

  Oligonucleotide–polyamine conjugates: Influence of length and position of 2′-attached polyamines on duplex stability and antisense effect

  摘要：

  Tethering cationic ligands to oligonucleotides results in zwitterionic molecules with often improved target affinity and better cell membrane permeation. Due to the ideal distance between cationic groups, polyamines are perfect counter ions for oligonucleotides. Using an easy and versatile procedure for attaching ligands to the 2'-position, polyamines were conjugated to distinct terminal and internal positions of oligonucleotides. With polyamines attached to terminal nucleosides, the affinity to complementary DNA or RNA strands increased with growing number of cationic amines. Tethering polyamines to an internal nucleoside of wild type DNA oligonucleotides resulted in a considerable decrease in duplex stability, but in phosphorothioates, no significant decrease was detected. Conjugates exhibited progressively higher target downregulation ability with increasing polyamine chain length in a human melanoma cell culture assay. (C) 2008 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2008.05.012

文献信息

• Polyamines and their use as antibacterial and sensitizing agents
  申请人：David Sunil A.

  公开号：US20070197658A1

  公开（公告）日：2007-08-23

  Polyamines with varying chain-lengths were evaluated for antimicrobial activity in order to test the hypothesis that these bis-cationic amphipathic compounds may also bind to and permeabilize intact Gram negative bacterial membranes. The compounds were found to possess significant antimicrobial activity and mediated via permeabilization of bacterial membranes. Homologated spermine, bis-acylated with C 8 or C 9 chains was found to profoundly sensitize E. coli to hydrophobic antibiotics such as rifampicin.

  多种链长的多胺被评估其抗微生物活性，以验证这些双阳离子两性化合物可能也结合并使革兰氏阴性细菌膜通透的假设。发现这些化合物具有显著的抗微生物活性，并通过细菌膜通透介导。经过烷基化的精胺，与C8或C9链双酰化，被发现能显著增加大肠杆菌对亲脂性抗生素如利福平的敏感性。
• Novel polyamine analogues as therapeutic and diagnostic agents
  申请人：ORIDIGM CORPORATION

  公开号：EP1085011A1

  公开（公告）日：2001-03-21

  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 disease 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.

  本发明揭示了具有比已知化合物低两个数量级的抑制常数的多胺转运抑制剂。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的有用药物，例如癌症和血管成形术后的损伤。揭示了获得多胺类似物的新的化学合成方法，包括制备组合多胺库。这些方法产生的类似物具有理想的诊断和研究测定和治疗活性。本发明的测定方法对于高通量筛选与多胺系统相互作用的药物发现目标非常有用。
• Plant protection formulation containing a copper-polyamine chelate
  申请人：BMS Micro-Nutrients N.V.

  公开号：EP1342413A1

  公开（公告）日：2003-09-10

  A plant protection formulation containing at least one Cu2+-containing compound as an active ingredient, characterised in that the active ingredient comprises an amount of at least one chelate of Cu2+ with a polyamine compound.

  一种植物保护制剂，含有至少一种含 Cu2+ 的化合物作为活性成分，其特征在于该活性成分包含一定量的至少一种 Cu2+ 与多胺化合物的螯合物。
• 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。
• Processes and host cells for genome, pathway, and biomolecular engineering
  申请人：enEvolv, Inc.

  公开号：US10370654B2

  公开（公告）日：2019-08-06

  The present disclosure provides compositions and methods for genomic engineering.

  本公开提供了基因组工程的组合物和方法。