7-chloro-4-{4-[2-(dipropylamino)ethyl]piperazin-1-yl}quinoline

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 7-chloro-4-{4-[2-(dipropylamino)ethyl]piperazin-1-yl}quinoline
• 英文别名: N-[2-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]ethyl]-N-propylpropan-1-amine
• 化学式: C₂₁H₃₁ClN₄
• 分子量: 374.957
• InChiKey: XSVMQJWGEGXSIX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  22.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  7-氯-4-(1-哌嗪基)喹啉 在 三乙胺 作用下， 以 甲醇 为溶剂， 反应 68.0h， 生成 7-chloro-4-{4-[2-(dipropylamino)ethyl]piperazin-1-yl}quinoline
  参考文献：
  名称：

  New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity

  摘要：

  Novel co-aminoacyl and -alkyl derivatives of 7-chloroquinolin-4-amine were prepared and their structures confirmed by NMR spectroscopy. Their antiprotozoal activities were examined in vitro against the sensitive NF54 strain as well as against the multiresistant K-1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). The results were compared with the activities of clinically used drugs. Their antitypanosomal activities were only moderate whereas their antiplasmodial activities looked very promising. Some were equal or slightly more active than chloroquine against the sensitive strain. However, in comparison to chloroquine, the activity of the new compounds was decreased much less in the resistant strain. Several possessed activity against both strains in low nanomolar concentration. (C) 2016 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2016.12.006

文献信息

• New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity
  作者：Johanna Faist、Clemens Hinteregger、Werner Seebacher、Robert Saf、Pascal Mäser、Marcel Kaiser、Robert Weis

  DOI：10.1016/j.bmc.2016.12.006

  日期：2017.2

  Novel co-aminoacyl and -alkyl derivatives of 7-chloroquinolin-4-amine were prepared and their structures confirmed by NMR spectroscopy. Their antiprotozoal activities were examined in vitro against the sensitive NF54 strain as well as against the multiresistant K-1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). The results were compared with the activities of clinically used drugs. Their antitypanosomal activities were only moderate whereas their antiplasmodial activities looked very promising. Some were equal or slightly more active than chloroquine against the sensitive strain. However, in comparison to chloroquine, the activity of the new compounds was decreased much less in the resistant strain. Several possessed activity against both strains in low nanomolar concentration. (C) 2016 Elsevier Ltd. All rights reserved.