N-(Piperidin-4-ylmethyl)propionamide | 886507-02-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: N-(Piperidin-4-ylmethyl)propionamide
• 英文别名: N-(piperidin-4-ylmethyl)propanamide
• CAS: 886507-02-4
• 化学式: C₉H₁₈N₂O
• 分子量: 170.255
• InChiKey: NBXUARPGNMORQJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(Piperidin-4-ylmethyl)propionamide 、 苯甲酰氯 在 三乙胺 作用下， 以 氯仿 为溶剂， 反应 24.0h， 以99%的产率得到N-[(1-benzoylpiperidin-4-yl)methyl]propanamide
  参考文献：
  名称：

  Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers

  摘要：

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.050
• 作为产物：
  描述：

  4-(propionylamino-methyl)-piperidine-1-carboxylic acid tert-butyl ester 在 盐酸 作用下， 以 乙酸乙酯 为溶剂， 反应 3.0h， 以74%的产率得到N-(Piperidin-4-ylmethyl)propionamide
  参考文献：
  名称：

  Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers

  摘要：

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.050

文献信息

• 2,5-DIKETOPIPERAZINES FOR THE TREATMENT OF OBESITY
  申请人：NOVO NORDISK A/S

  公开号：EP1572669A2

  公开（公告）日：2005-09-14
• US5189045A
  申请人：——

  公开号：US5189045A

  公开（公告）日：1993-02-23
• [EN] COMPOUNDS FOR USE IN TREATING OBESITY<br/>[FR] COMPOSES DESTINES AU TRAITEMENT DE L'OBESITE
  申请人：NOVO NORDISK AS

  公开号：WO2004048345A2

  公开（公告）日：2004-06-10

  The present invention relates to novel compounds of the general formula (I) as well as any optical or geometric isomer or tautomer form thereof, or a pharmaceutically acceptable salt thereof, as agonists of melanocortin receptors, such as agonists of the MC4 receptor. The compounds may for instance be used in the treatment of obesity.
• Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
  作者：Elisabetta Martini、Carla Ghelardini、Silvia Dei、Luca Guandalini、Dina Manetti、Michele Melchiorre、Monica Norcini、Serena Scapecchi、Elisabetta Teodori、Maria Novella Romanelli

  DOI：10.1016/j.bmc.2007.10.050

  日期：2008.2.1

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.