DL-4-azido-3-tert-butoxycarbonylamino-butyric acid methyl ester | 942297-61-2

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: DL-4-azido-3-tert-butoxycarbonylamino-butyric acid methyl ester
• 英文别名: 4-Azido-3-tert-butoxycarbonylamino-butyric acid methyl ester；methyl 4-azido-3-[(2-methylpropan-2-yl)oxycarbonylamino]butanoate
• CAS: 942297-61-2
• 化学式: C₁₀H₁₈N₄O₄
• 分子量: 258.277
• InChiKey: ZOLUQSYOHPFOAI-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：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  79
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  DL-4-azido-3-tert-butoxycarbonylamino-butyric acid methyl ester 在 palladium 10% on activated carbon 、 氢气 、 三乙胺 、 N,N'-二环己基碳二亚胺 、 lithium hydroxide 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 水 为溶剂， 反应 30.0h， 生成 di-t-butyl 4-oxo-4-(piperazin-1-yl)butane-1,2-diyldicarbamate
  参考文献：
  名称：

  Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease

  摘要：

  An important part of pathogenesis of Alzheimer's disease (AD) is attributed to the contribution of AGE (Advanced Glycation Endproducts) and ALE (Advanced Lipid peroxidation Endproducts). In order to attenuate the progression of AD, we designed a new type of molecules that consist of two trapping parts for reactive carbonyl species (RCS) and reactive oxygen species (ROS), precursors of AGE and ALE, respectively. These molecules also chelate transition metals, the promoters of ROS formation. In this paper, synthesis of the new AGE/ALE inhibitors and evaluation of their physicochemical and biological properties (carbonyl trapping capacity, antioxidant activity, Cu2+-chelating capacity, cytotoxicity and protective effect against in vitro MGO-induced apoptosis in the model AD cell-line PC12) are described. It is found that compounds 40b and 51e possess promising therapeutic potentials for treating AD. (C) 2016 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2016.04.069
• 作为产物：
  描述：

  2-(叔丁氧基羰基氨基)-4-甲氧基-4-氧代丁酸 在 sodium tetrahydroborate 、 sodium azide 、 三乙胺 作用下， 以 四氢呋喃 、 乙醇 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 5.0h， 生成 DL-4-azido-3-tert-butoxycarbonylamino-butyric acid methyl ester
  参考文献：
  名称：

  Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease

  摘要：

  An important part of pathogenesis of Alzheimer's disease (AD) is attributed to the contribution of AGE (Advanced Glycation Endproducts) and ALE (Advanced Lipid peroxidation Endproducts). In order to attenuate the progression of AD, we designed a new type of molecules that consist of two trapping parts for reactive carbonyl species (RCS) and reactive oxygen species (ROS), precursors of AGE and ALE, respectively. These molecules also chelate transition metals, the promoters of ROS formation. In this paper, synthesis of the new AGE/ALE inhibitors and evaluation of their physicochemical and biological properties (carbonyl trapping capacity, antioxidant activity, Cu2+-chelating capacity, cytotoxicity and protective effect against in vitro MGO-induced apoptosis in the model AD cell-line PC12) are described. It is found that compounds 40b and 51e possess promising therapeutic potentials for treating AD. (C) 2016 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2016.04.069

文献信息

• Heteroarylpyrrolopyridinones active as kinase inhibitors
  申请人：Vanotti Ermes

  公开号：US20070142415A1

  公开（公告）日：2007-06-21

  Compounds represented by formula (I) wherein A, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification or a pharmaceutically acceptable salt or solvate thereof, compositions thereof, and methods of use thereof.

  由式（I）表示的化合物 其中A，R1，R2，R3，R4，R5和R6如规范中定义，或其药用可接受盐或溶剂，其组合物和使用方法。
• HETEROARYLPYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS
  申请人：Nerviano Medical Sciences S.r.l.

  公开号：EP1963319B1

  公开（公告）日：2012-04-11
• US7618982B2
  申请人：——

  公开号：US7618982B2

  公开（公告）日：2009-11-17
• Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease
  作者：Elodie Lohou、N. André Sasaki、Agnès Boullier、Pascal Sonnet

  DOI：10.1016/j.ejmech.2016.04.069

  日期：2016.10

  An important part of pathogenesis of Alzheimer's disease (AD) is attributed to the contribution of AGE (Advanced Glycation Endproducts) and ALE (Advanced Lipid peroxidation Endproducts). In order to attenuate the progression of AD, we designed a new type of molecules that consist of two trapping parts for reactive carbonyl species (RCS) and reactive oxygen species (ROS), precursors of AGE and ALE, respectively. These molecules also chelate transition metals, the promoters of ROS formation. In this paper, synthesis of the new AGE/ALE inhibitors and evaluation of their physicochemical and biological properties (carbonyl trapping capacity, antioxidant activity, Cu2+-chelating capacity, cytotoxicity and protective effect against in vitro MGO-induced apoptosis in the model AD cell-line PC12) are described. It is found that compounds 40b and 51e possess promising therapeutic potentials for treating AD. (C) 2016 Elsevier Masson SAS. All rights reserved.