EM106

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: EM106
• 英文别名: 1-(4-Propan-2-ylsulfonylpiperazin-1-yl)ethanone
• 化学式: C₉H₁₈N₂O₃S
• 分子量: 234.32
• InChiKey: MIQUZTZCHPJKLF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  66.1
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1-乙酰哌嗪 、 异丙基磺酰氯 在 三乙胺 作用下， 以 乙腈 为溶剂， 反应 24.0h， 以66%的产率得到EM106
  参考文献：
  名称：

  Structure–activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs

  摘要：

  Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2003.10.025

文献信息

• SEPIAPTERIN REDUCTASE INHIBITORS
  申请人：QUARTET MEDICINE, INC.

  公开号：US20170096435A1

  公开（公告）日：2017-04-06

  Inhibitors of sepiapterin reductase and uses of sepiapterin reductase inhibitors in analgesia, treatment of acute and chronic pain, anti-inflammation, and immune cell regulation are disclosed.
• Structure–activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
  作者：Serena Scapecchi、Elisabetta Martini、Dina Manetti、Carla Ghelardini、Cecilia Martelli、Silvia Dei、Nicoletta Galeotti、Luca Guandalini、Maria Novella Romanelli、Elisabetta Teodori

  DOI：10.1016/j.bmc.2003.10.025

  日期：2004.1

  Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg. (C) 2003 Elsevier Ltd. All rights reserved.