N-(4-(dimethylamino)-but-2-enyl)-7-chloroquinolin-4-amine | 21373-55-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-(4-(dimethylamino)-but-2-enyl)-7-chloroquinolin-4-amine
• 英文别名: N-(7-chloroquinolin-4-yl)-N',N'-diethylbut-2-yne-1,4-diamine
• CAS: 21373-55-7
• 化学式: C₁₇H₂₀ClN₃
• 分子量: 301.819
• InChiKey: FXFZQWXJXDXZGX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  28.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  聚合甲醛 、 7-chloro-N-(prop-2-yn-1-yl)quinolin-4-amine 、 二乙胺 在 copper(l) iodide 作用下， 以 乙醇 为溶剂， 以40 %的产率得到N-(4-(dimethylamino)-but-2-enyl)-7-chloroquinolin-4-amine
  参考文献：
  名称：

  COMPOUND DERIVED FROM QUINOLINE, USE OF A COMPOUND, COMPOSITION AND METHOD FOR THE TREATMENT OR PROPHYLAXIS OF A CONDITION CAUSED BY A BLOOD PARASITE

  摘要：

  Despite recent efforts to eradicate malaria worldwide, this parasitic disease is still considered a major public health problem, with a total of 219 million malaria cases and 435,000 deaths in 2017 After a decade of use, however, resistance to CQ has emerged in some locations, including Southeast Asia, South America, and the Western Pacific region, spreading progressively into malaria-endemic areas, including Africa, where increases in malaria mortality have been observed. This has led, in recent years, to the adoption of artemisinin-based combination therapies. Artemisinin-based combination therapies remain effective in most parts of the world, but recent cases of resistance in Southeast Asia call for new approaches and especially new drugs to treat malaria. Thus, the present invention features CQ analogues of Formula (I) that exhibited high activity against CQ-sensitive and CQ-resistant blood parasites and were also active in mice. The present invention also provides pharmaceutical compositions comprising the compounds of Formula (I), use of said compounds, and methods for treating conditions caused by blood parasites.

  公开号：

  US20220332685A1