1-acetyl-4-benzoylpiperazine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-acetyl-4-benzoylpiperazine
• 英文别名: 1-(4-benzoylpiperazin-1-yl)ethanone；4-Acetyl-1-benzoylpiperazine
• 化学式: C₁₃H₁₆N₂O₂
• mdl: MFCD10048079
• 分子量: 232.282
• InChiKey: MWAMAMKEZQPIGU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.384
• 拓扑面积：
  40.6
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  在 双氧水 作用下， 反应 1.5h， 生成 1-acetyl-4-benzoylpiperazine
  参考文献：
  名称：

  Hydrogen peroxide mediated efficient amidation and esterification of aldehydes: Scope and selectivity

  摘要：

  一种利用过氧化氢作为氧化剂实现醛的酰胺化和酯化的高效方法已被开发出来。在温和条件下，环状胺和伯醇能选择性地与芳香醛发生反应，生成相应的酰胺和酯。

  DOI：

  10.1039/c1gc16041a

文献信息

• BUFADIENOLIDE DERIVATIVES, PREPARING PROCESS THEREOF, COMPOSITION COMPRISING THE SAME AND THE USE THEREOF
  申请人：Hu Lihong

  公开号：US20130005696A1

  公开（公告）日：2013-01-03

  The present invention provides a class of bufadienolide derivatives representing by the following formula I or pharmaceutically acceptable salts thereof, the preparing process thereof, pharmaceutical composition comprising the same and the use thereof. The bufadienolide derivatives have inhibitory activities against human-derived tumor cell lines, and thus can be used as a drug for treating malignancies.

  本发明提供了一类以以下公式I表示的蟾毒甾醇衍生物或其药用盐，其制备方法，包含相同的药物组合物以及其用途。蟾毒甾醇衍生物对人源肿瘤细胞系具有抑制活性，因此可用作治疗恶性肿瘤的药物。
• Novel Choline Kinase Inhibitors
  申请人：ZECH Stephan G.

  公开号：US20160024024A1

  公开（公告）日：2016-01-28

  This invention relates to compounds of the general formula (I): in which the variable groups are as identified herein, and to preparation and use of the compounds.

  本发明涉及一般式（I）的化合物，其中变量基团如本文所述，并涉及所述化合物的制备和使用。
• Piperazine derivatives possesing nootropic activity
  申请人：Universita Degli Studi di Firenze

  公开号：EP1118612A1

  公开（公告）日：2001-07-25

  Piperazine derivatives with general structure (I) are described. There: R1 can be H or C1-5 alkyl; R2 and R3 are both H or linked together to form a bridge -CH2-; X can be H, F, OCH3, Cl, NO2, NH2, CH3; Z can be CO, SO2. The compounds described above are endowed with an interesting nootropic activity that makes them suitable to treat neurodegenerative diseases such as Alzheimer's disease.

  描述了具有一般结构 (I) 的哌嗪衍生物。其中 R1 可以是 H 或 C1-5 烷基； R2 和 R3 都是 H 或连接在一起形成桥 -CH2-； X可以是H、F、OCH3、Cl、NO2、NH2、CH3； Z 可以是 CO、SO2。 上述化合物具有有趣的促智活性，适合治疗神经退行性疾病，如阿尔茨海默病。
• Molecular Simplification of 1,4-Diazabicyclo[4.3.0]nonan-9-ones Gives Piperazine Derivatives That Maintain High Nootropic Activity
  作者：Dina Manetti、Carla Ghelardini、Alessandro Bartolini、Silvia Dei、Nicoletta Galeotti、Fulvio Gualtieri、Maria Novella Romanelli、Elisabetta Teodori

  DOI：10.1021/jm000972h

  日期：2000.11.1

  Several 4-substituted 1-acylpiperazines, obtained by molecular simplification of 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones, have been synthesized and tested in vivo on the mouse passive avoidance test, to evaluate their nootropic activity. The results show that, apparently, an N-acylpiperazine group can mimic the 2-pyrrolidinone ring of 1,4-diazabicyclo[4.3.0]nonan-9-one, as the compounds of the new series maintain high nootropic activity. Moreover molecular simplification produces more clear-cut structure-activity relationships with respect to the parent series. The mechanism of action also appears to be similar in the two series. In fact, although the molecular mechanism remains to be elucidated, the most potent compound of each class (DM232 and 13, DM235) is able to increase acetylcholine release in rat brain. Piperazine derivatives represent a new class of nootropic drugs with an in vivo pharmacological profile very similar to that of piracetam, showing much higher potency with respect to the reference compound. Among the compounds studied, 13 (DM235) shows outstanding potency, being active at a dose of 0.001 mg kg(-1) sc.
• Novel Sunifiram-carbamate hybrids as potential dual acetylcholinesterase inhibitor and NMDAR co-agonist: simulation-guided analogue design and pharmacological screening
  作者：Khalid A. Agha、Nader E. Abo-Dya、Abdul Rashid Issahaku、Clement Agoni、Mahmoud E. S. Soliman、Eatedal H. Abdel-Aal、Zakaria K. Abdel-Samii、Tarek S. Ibrahim

  DOI：10.1080/14756366.2022.2068147

  日期：2022.12.31