N-Trityl-N'-[4-(trityl-amino)-butyl]-butane-1,4-diamine | 622839-31-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: N-Trityl-N'-[4-(trityl-amino)-butyl]-butane-1,4-diamine
• CAS: 622839-31-0
• 化学式: C₄₆H₄₉N₃
• 分子量: 643.915
• InChiKey: JMMFGYGBWYUOAB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  9.3
• 重原子数：
  49.0
• 可旋转键数：
  18.0
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  36.09
• 氢给体数：
  3.0
• 氢受体数：
  3.0

反应信息

• 作为反应物：
  描述：

  N-Trityl-N'-[4-(trityl-amino)-butyl]-butane-1,4-diamine 在 4-二甲氨基吡啶 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 5.5h， 生成
  参考文献：
  名称：

  Synthesis of Novel G Factor or Chloroquine-Artemisinin Hybrids and Conjugates with Potent Antiplasmodial Activity

  摘要：

  A series of novel hybrids of artemisinin (ART) with either a phytormone endoperoxide G factor analogue (GMeP) or chloroquine (CQ) and conjugates of the same compounds with the polyamines (PAs), spermidine (Spd), and homospermidine (Hsd) were synthesized and their antiplasmodial activity was evaluated using the CQ-resistant P. falciparum FcB1/Colombia strain. The ART-GMeP hybrid 5 and compounds 9 and 10 which are conjugates of Spd and Hsd with two molecules of ART and one molecule of GMeP, were the most potent with IC50 values of 2.6, 8.4, and 10.6 nM, respectively. The same compounds also presented the highest selectivity indexes against the primary human fibroblast cell line AB943 ranging from 16 372 for the hybrid 5 to 983 for the conjugate 10 of Hsd.

  DOI：

  10.1021/acsmedchemlett.9b00669
• 作为产物：
  描述：

  4,4'-[(苯基甲基)亚氨基]二丁腈 在 palladium dihydroxide 、 镍 sodium hydroxide 、 氢气 、 三乙胺 作用下， 以 乙醇 、 氯仿 为溶剂， 生成 N-Trityl-N'-[4-(trityl-amino)-butyl]-butane-1,4-diamine
  参考文献：
  名称：

  Xylylated dimers of putrescine and polyamines: influence of the polyamine backbone on spermidine transport inhibition

  摘要：

  Dimeric norspermidine and spermidine derivatives are strong competitive inhibitors of polyamine transport. A xylyl tether was used for the dimerization of various triamines and spermine via a secondary amino group, and of putrescine via an ether or an amino group. Dimerization of putrescine moieties potentiates their ability to compete against spermidine transport to a much greater extent than for triamine dimers. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00668-1

文献信息

• Synthesis and Antiplasmodial Activity of Novel Fosmidomycin Derivatives and Conjugates with Artemisinin and Aminochloroquinoline
  作者：Despina Palla、Antonia I. Antoniou、Michel Baltas、Christophe Menendez、Philippe Grellier、Elisabeth Mouray、Constantinos M. Athanassopoulos

  DOI：10.3390/molecules25204858

  日期：——

  the development of drug resistance by Plasmodium falciparum. The antibiotic fosmidomycin (FSM) is also known for its antimalarial activity by targeting the non-mevalonate isoprenoid synthesis pathway, which is essential for the malaria parasites but is absent in mammalians. In this study, we synthesized and evaluated against the chloroquine-resistant P. falciparum FcB1/Colombia strain, a series of FSM

  尽管作出了许多努力，但疟疾仍然是全世界最成问题的传染病之一，主要是由于恶性疟原虫产生了耐药性。抗生素磷磷霉素（FSM）还具有靶向非甲羟戊酸类异戊二烯合成途径的抗疟疾活性，该途径对疟疾寄生虫至关重要，但在哺乳动物中却不存在。在这项研究中，我们合成并针对抗氯喹的恶性疟原虫FcB1 / Colombia菌株，一系列FSM类似物，衍生物和与其他抗疟疾药物（如青蒿素（ART）和氨基氯喹啉（ACQ））的缀合物进行了合成和评估。生物学评估发现，有四种新化合物具有比FSM更高的抗疟活性：两种FSM-ACQ衍生物和两种FSM-ART结合物，其有效活性是FSM的3.5-5.4和41.5-23.1倍，