2-N-(4-ethoxyphenyl)pyridine-2,3,5-triamine | 1421589-74-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-N-(4-ethoxyphenyl)pyridine-2,3,5-triamine
• CAS: 1421589-74-3
• 化学式: C₁₃H₁₆N₄O
• 分子量: 244.296
• InChiKey: PDJNDWZXZSAROH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  86.2
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-N-(4-ethoxyphenyl)pyridine-2,3,5-triamine 以 甲醇 为溶剂， 反应 6.0h， 生成
  参考文献：
  名称：

  Discovery and optimization of potent broad-spectrum arenavirus inhibitors derived from benzimidazole and related heterocycles

  摘要：

  A series of potent arenavirus inhibitors sharing a benzimidazole core were previously reported by our group. SAR studies were expanded beyond the previous analysis, which involved the attached phenyl rings and methylamino linker portion, to include modifications focused on the benzimidazole core. These changes included the introduction of various substituents to the bicyclic benzimidazole ring system along with alternate core heterocycles. Many of the analogs containing alternate nitrogen-based bicyclic ring systems were found to retain antiviral potency compared to the benzimidazole series from which we derived our lead compound, ST-193. In fact, 21h, built on an imidazopyridine core, possessed a near tenfold increase in potency against Lassa virus pseudotypes compared to ST-193. As found with the benzimidazole series, broad-spectrum arenavirus activity was also observed for a number of the analogs discovered during this study. (c) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.11.093
• 作为产物：
  描述：

  2-氟-3,5-二硝基吡啶 在 palladium 10% on activated carbon 、 氢气 、 caesium carbonate 作用下， 以 四氢呋喃 、 乙酸乙酯 为溶剂， 生成 2-N-(4-ethoxyphenyl)pyridine-2,3,5-triamine
  参考文献：
  名称：

  Antiviral drugs for treatment of Arenavirus infection

  摘要：

  本发明涉及用于治疗病毒感染的化合物、方法和药物组合物，通过在治疗上有效剂量下给予某些化合物来进行治疗。还公开了制备这些化合物的方法以及使用这些化合物和药物组合物的方法。特别是针对由Arenavirus家族引起的病毒感染的治疗和预防，如拉萨热、阿根廷出血热、玻利维亚出血热和委内瑞拉出血热。

  公开号：

  US09096597B2

文献信息

• Discovery and optimization of potent broad-spectrum arenavirus inhibitors derived from benzimidazole and related heterocycles
  作者：James R. Burgeson、Amy L. Moore、Dima N. Gharaibeh、Ryan A. Larson、Natasha R. Cerruti、Sean M. Amberg、Dennis E. Hruby、Dongcheng Dai

  DOI：10.1016/j.bmcl.2012.11.093

  日期：2013.2

  A series of potent arenavirus inhibitors sharing a benzimidazole core were previously reported by our group. SAR studies were expanded beyond the previous analysis, which involved the attached phenyl rings and methylamino linker portion, to include modifications focused on the benzimidazole core. These changes included the introduction of various substituents to the bicyclic benzimidazole ring system along with alternate core heterocycles. Many of the analogs containing alternate nitrogen-based bicyclic ring systems were found to retain antiviral potency compared to the benzimidazole series from which we derived our lead compound, ST-193. In fact, 21h, built on an imidazopyridine core, possessed a near tenfold increase in potency against Lassa virus pseudotypes compared to ST-193. As found with the benzimidazole series, broad-spectrum arenavirus activity was also observed for a number of the analogs discovered during this study. (c) 2012 Elsevier Ltd. All rights reserved.
• Antiviral drugs for treatment of Arenavirus infection
  申请人：Kineta Four, LLC

  公开号：US09096597B2

  公开（公告）日：2015-08-04

  Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.

  本发明涉及用于治疗病毒感染的化合物、方法和药物组合物，通过在治疗上有效剂量下给予某些化合物来进行治疗。还公开了制备这些化合物的方法以及使用这些化合物和药物组合物的方法。特别是针对由Arenavirus家族引起的病毒感染的治疗和预防，如拉萨热、阿根廷出血热、玻利维亚出血热和委内瑞拉出血热。