2-[4-[(6-甲氧基-4-甲基喹啉-8-基)氨基]己基]异吲哚-1,3-二酮 | 76367-79-8

• 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
• 中文名称: 2-[4-[(6-甲氧基-4-甲基喹啉-8-基)氨基]己基]异吲哚-1,3-二酮
• 英文名称: 8-<(1-ethyl-4-phthalimidobutyl)amino>-6-methoxy-4-methylquinoline
• 英文别名: 8-[(1-Ethyl-4-phthalimido-butyl)amino]-6-methoxy-4-methylquinoline；2-[4-[(6-methoxy-4-methylquinolin-8-yl)amino]hexyl]isoindole-1,3-dione
• CAS: 76367-79-8
• 化学式: C₂₅H₂₇N₃O₃
• 分子量: 417.508
• InChiKey: NTNDOHCEODMOBB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  71.5
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-[4-[(6-甲氧基-4-甲基喹啉-8-基)氨基]己基]异吲哚-1,3-二酮 在 一水合肼 作用下， 以 乙醇 为溶剂， 反应 6.0h， 生成 8-<(1-ethyl-4-aminobutyl)amino>-6-methoxy-4-methylquinoline
  参考文献：
  名称：

  Synthesis and antimalarial activity of 8-[(1-alkyl-4-aminobutyl)amino]-6-methoxy-4-methylquinolines

  摘要：

  Three analogues of the causal prophylactic antimalarial primaquine were prepared and their antimalarial activity was evaluated. 8-[(1-Ethyl-4-aminobutyl)amino]-6-methoxy-4-methylquinoline (2a) demonstrated activity against Plasmodium berghei in mice at 20 mg/kg, with all animals cured at 320 mg/kg, and is without toxicity at 640 mg/kg. It also possessed outstanding causal prophylactic activity against Plasmodium cynomolgi in rhesus monkeys at very low dosages.

  DOI：

  10.1021/jm00134a019
• 作为产物：
  描述：

  1,4-二溴己烷 在 二异丙胺 作用下， 以 乙二醇乙醚 、 乙醇 、 丙酮 为溶剂， 反应 63.0h， 生成 2-[4-[(6-甲氧基-4-甲基喹啉-8-基)氨基]己基]异吲哚-1,3-二酮
  参考文献：
  名称：

  Synthesis and antimalarial activity of 8-[(1-alkyl-4-aminobutyl)amino]-6-methoxy-4-methylquinolines

  摘要：

  Three analogues of the causal prophylactic antimalarial primaquine were prepared and their antimalarial activity was evaluated. 8-[(1-Ethyl-4-aminobutyl)amino]-6-methoxy-4-methylquinoline (2a) demonstrated activity against Plasmodium berghei in mice at 20 mg/kg, with all animals cured at 320 mg/kg, and is without toxicity at 640 mg/kg. It also possessed outstanding causal prophylactic activity against Plasmodium cynomolgi in rhesus monkeys at very low dosages.

  DOI：

  10.1021/jm00134a019

文献信息

• YAN SHOU-JEN; CHIEN PING-LU; CHENG C. C., J. MED. CHEM.,1981, 24, NO 2, 215-217
  作者：YAN SHOU-JEN、 CHIEN PING-LU、 CHENG C. C.

  DOI：——

  日期：——
• Synthesis and antimalarial activity of 8-[(1-alkyl-4-aminobutyl)amino]-6-methoxy-4-methylquinolines
  作者：Shou-Jen Yan、Ping-Lu Chien、C. C. Cheng

  DOI：10.1021/jm00134a019

  日期：1981.2

  Three analogues of the causal prophylactic antimalarial primaquine were prepared and their antimalarial activity was evaluated. 8-[(1-Ethyl-4-aminobutyl)amino]-6-methoxy-4-methylquinoline (2a) demonstrated activity against Plasmodium berghei in mice at 20 mg/kg, with all animals cured at 320 mg/kg, and is without toxicity at 640 mg/kg. It also possessed outstanding causal prophylactic activity against Plasmodium cynomolgi in rhesus monkeys at very low dosages.