2-(1-(4-acetylphenyl)piperidin-4-yl)acetic acid | 923945-26-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(1-(4-acetylphenyl)piperidin-4-yl)acetic acid
• 英文别名: [1-(4-acetyl-phenyl)-piperidin-4-yl]-acetic acid；2-[1-(4-acetylphenyl)piperidin-4-yl]acetic acid
• CAS: 923945-26-0
• 化学式: C₁₅H₁₉NO₃
• 分子量: 261.321
• InChiKey: OFKFKOUCGDKARR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  57.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(1-(4-acetylphenyl)piperidin-4-yl)acetic acid 、 1-环戊基哌嗪 在 (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 2-[1-(4-acetyl-phenyl)-piperidin-4-yl]-1-(4-cyclobutyl-piperazin-1-yl)-ethanone
  参考文献：
  名称：

  WO2007/16496

  摘要：

  公开号：
• 作为产物：
  描述：

  [1-(4-acetyl-phenyl)-piperidin-4-yl]-acetic acid ethyl ester 在 lithium hydroxide 、 水 作用下， 以 四氢呋喃 为溶剂， 生成 2-(1-(4-acetylphenyl)piperidin-4-yl)acetic acid
  参考文献：
  名称：

  WO2007/16496

  摘要：

  公开号：

文献信息

• 2-(Piperidin-4-yl)acetamides as Potent Inhibitors of Soluble Epoxide Hydrolase with Anti-Inflammatory Activity
  作者：Juan Martín-López、Sandra Codony、Clara Bartra、Christophe Morisseau、María Isabel Loza、Coral Sanfeliu、Bruce D. Hammock、José Brea、Santiago Vázquez

  DOI：10.3390/ph14121323

  日期：——

  The pharmacological inhibition of soluble epoxide hydrolase (sEH) has been suggested as a potential therapy for the treatment of pain and inflammatory diseases through the stabilization of endogenous epoxyeicosatrienoic acids. Numerous potent sEH inhibitors (sEHI) have been developed, however many contain highly lipophilic substituents limiting their availability. Recently, a new series of benzohomoadamantane-based ureas endowed with potent inhibitory activity for the human and murine sEH was reported. However, their very low microsomal stability prevented further development. Herein, a new series of benzohomoadamantane-based amides were synthetized, fully characterized, and evaluated as sEHI. Most of these amides were endowed with excellent inhibitory potencies. A selected compound displayed anti-inflammatory effects with higher effectiveness than the reference sEHI, TPPU.

  可溶性环氧脂水解酶（sEH）的药理抑制已被提出作为通过稳定内源性环氧三烯酸治疗疼痛和炎症性疾病的潜在疗法。已经开发了许多有效的sEH抑制剂（sEHI），然而许多含有高脂溶性取代基的化合物限制了它们的可用性。最近，报道了一系列基于苯并环辛烷基脲的新型化合物，具有对人类和小鼠sEH的强大抑制活性。然而，它们的低微粒体稳定性阻碍了进一步的开发。在这里，合成了一系列基于苯并环辛烷基酰胺的新化合物，进行了全面的表征，并作为sEHI进行了评估。其中大多数酰胺具有出色的抑制活性。一种选定的化合物显示出抗炎效果，其效果比参考的sEHI TPPU 更高。
• Dipiperazinyl ketones and related analogues
  申请人：Xie Linghong

  公开号：US20070049571A1

  公开（公告）日：2007-03-01

  Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

  提供了二吡咯啉酮和相关类似物，以及它们的制备和使用方法。这些化合物通常可用于体内或体外调节组胺H3受体的配体结合，并特别适用于治疗人类、家养伴侣动物和家畜动物的各种疾病。提供了药物组合物和治疗方法，以及使用这些配体检测组胺H3受体的方法（例如，受体定位研究）。
• Bi-functional complexes and methods for making and using such complexes
  申请人：Gouliaev Alex Haahr

  公开号：US11225655B2

  公开（公告）日：2022-01-18

  The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

  本发明涉及一种合成双功能复合物的方法，该复合物包括分子部分和识别分子部分的识别寡核苷酸部分。根据本发明的合成方法的一部分优选在一种或多种有机溶剂中进行，此时包含可选保护标签或寡核苷酸标识符的新生双功能复合物与固体支持物相连接，合成方法的另一部分优选在适合于将寡核苷酸标签酶加到溶液中的新生双功能复合物的条件下进行。
• DIPIPERAZINYL KETONES AND RELATED ANALOGUES
  申请人：NEUROGEN CORPORATION

  公开号：EP1909797A2

  公开（公告）日：2008-04-16
• BI-FUNCTIONAL COMPLEXES AND METHODS FOR MAKING AND USING SUCH COMPLEXES
  申请人：Nuevolution A/S

  公开号：EP2558577B1

  公开（公告）日：2018-12-12