(E)-(3,4,5-trimethoxyphenyl)methylidenehydrazine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: (E)-(3,4,5-trimethoxyphenyl)methylidenehydrazine
• 化学式: C₁₀H₁₄N₂O₃
• 分子量: 210.233
• InChiKey: ZWCPJPDZBZBJNV-WUXMJOGZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  66.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (E)-(3,4,5-trimethoxyphenyl)methylidenehydrazine 、 2-(4-phenyl-1H-1,2,3-triazol-1-yl)acetic acid 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.58h， 以65.31%的产率得到(E)-2-(4-phenyl-1H-1,2,3-triazol-1-yl)-N'-(3,4,5-trimethoxybenzylidene)acetohydrazide
  参考文献：
  名称：

  Synthesis and biological evaluation of novel (E)-N'-benzylidene hydrazides as novel c-Met inhibitors through fragment based virtual screening

  摘要：

  C-Met plays a crucial role in the development and progression of neoplastic disease. Type II c-Met inhibitors recognise the inactive DFG-out conformation of the kinase, result in better anti-tumour effects due to synergistic effect against the other kinases. According to our previous works, an (E)-N'-benzylidene group was selected as the initial fragment. Two series of (E)-N'-benzylidene hydrazides were designed by fragment growth method. The inhibitory activities were in vitro investigated against c-Met and VEGFR-2. Compound 10b exhibited the most potent inhibitory activity against the c-Met inhibitor (IC50 = 0.37 nM). Compound 11b exhibited multi-target c-Met kinase inhibitory activity as a potential type II c-Met inhibitor (IC50 = 3.41 nM against c-Met; 25.34 nM against VEGFR-2). The two compounds also demonstrate the feasibility of fragment-based virtual screening method for drug discovery.

  DOI：

  10.1080/14756366.2019.1702655
• 作为产物：
  描述：

  3,4,5-三甲氧基苯甲醛 在 一水合肼 作用下， 以 水 为溶剂， 反应 5.0h， 生成 (E)-(3,4,5-trimethoxyphenyl)methylidenehydrazine
  参考文献：
  名称：

  Synthesis and biological evaluation of novel (E)-N'-benzylidene hydrazides as novel c-Met inhibitors through fragment based virtual screening

  摘要：

  C-Met plays a crucial role in the development and progression of neoplastic disease. Type II c-Met inhibitors recognise the inactive DFG-out conformation of the kinase, result in better anti-tumour effects due to synergistic effect against the other kinases. According to our previous works, an (E)-N'-benzylidene group was selected as the initial fragment. Two series of (E)-N'-benzylidene hydrazides were designed by fragment growth method. The inhibitory activities were in vitro investigated against c-Met and VEGFR-2. Compound 10b exhibited the most potent inhibitory activity against the c-Met inhibitor (IC50 = 0.37 nM). Compound 11b exhibited multi-target c-Met kinase inhibitory activity as a potential type II c-Met inhibitor (IC50 = 3.41 nM against c-Met; 25.34 nM against VEGFR-2). The two compounds also demonstrate the feasibility of fragment-based virtual screening method for drug discovery.

  DOI：

  10.1080/14756366.2019.1702655

文献信息

• Combination of antioxidant substances for the treatment of alzheimer's disease
  申请人：Colba R & D Inc.

  公开号：US20030158237A1

  公开（公告）日：2003-08-21

  Disclosed is a pharmaceutical composition for the treatment of cognitive symptoms caused by Alzheimer's disease in a mammal. This composition comprising vitamin E, quercitin, caffeic acid, nicotinic acid or derivatives and/or analog thereof, and a pharmaceutically acceptable excipient.

  本发明公开了一种药物组合物，用于治疗由阿尔茨海默病引起的哺乳动物认知症状。该组合物包含维生素 E、槲皮素、咖啡酸、烟酸或其衍生物和/或类似物，以及药学上可接受的赋形剂。