2-(4-fluorophenyl)-2-(methylamino)cyclohexan-1-one | 2639570-44-6

• 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: 2-(4-fluorophenyl)-2-(methylamino)cyclohexan-1-one
• 英文别名: 2-(4-Fluorophenyl)-2-(methylamino)cyclohexanone
• CAS: 2639570-44-6
• 化学式: C₁₃H₁₆FNO
• 分子量: 221.275
• InChiKey: GLHWPYBETIKGHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-(4-氟苯基)环己酮 在 ammonium cerium (IV) nitrate 、 六氟异丙醇 、 copper diacetate 、 溶剂黄146 、 锌 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 36.0h， 生成 2-(4-fluorophenyl)-2-(methylamino)cyclohexan-1-one
  参考文献：
  名称：

  [EN] ARYLCYCLOHEXYLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PSYCHIATRIC DISORDERS
  [FR] DÉRIVÉS ARYLCYCLOHEXYLAMINE ET LEUR UTILISATION DANS LE TRAITEMENT DE TROUBLES PSYCHIATRIQUES

  摘要：

  本文提供了芳基环己胺衍生物及其在治疗精神疾病中的用途。

  公开号：

  WO2021134086A1

文献信息

• Arylcyclohexylamine derivatives and their use in the treatment of psychiatric disorders
  申请人：Gilgamesh Pharmaceuticals, Inc.

  公开号：US11344510B2

  公开（公告）日：2022-05-31

  Provided herein are arylcyclohexylamine derivatives and their use in the treatment of psychiatric disorders.

  本文提供的是芳基环己胺衍生物及其在治疗精神疾病中的用途。
• Discovery of novel ketamine‐inspired derivatives as a protective agent against renal ischemic/reperfusion injury in Wistar rats
  作者：Li Zhu、Yin Zhang

  DOI：10.1111/cbdd.14011

  日期：2022.7

  AbstractRenal ischemia‐reperfusion (I/R) injury is a limiting factor for the success of renal grafts and is deemed greatly responsible for the mortality. A novel series of ketamine‐inspired compounds was synthesized and subjected to NF‐ĸB transcriptional inhibitory activity in LPS‐stimulated RAW264.7 cells, where entire set of compounds showed mild‐to‐moderate significant NF‐ĸB transcriptional inhibitory activity (IC50 6.53–67.52 µM). Compound 6d showed highest inhibitory activity among the tested series (IC50 2.62 µM) and found more potent as compared to ketamine as standard. The effect of compound 6d was further quantified in I/R injury in Wistar rats, where it dose‐dependently improves kidney function of rats with significant amelioration of kidney injury as suggested by histopathologic examination of renal tissues. It further showed reduction in the generation of pro‐inflammatory cytokines and improves the antioxidant status of experimental rats. Compound 6d inhibited apoptosis and increases the expression of Bcl2 and decreases Bax, and cleaved caspase‐3 level. It further reduces TLR‐4 and NF‐κB expression in renal cells of rats, with increases in IκB‐α level in Western blot analysis as compared to I/R group. In summary, our current study showed the development of a novel class of ketamine‐inspired derivatives against renal ischemia/reperfusion injury.
• ARYLCYCLOHEXYLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PSYCHIATRIC DISORDERS
  申请人：Gilgamesh Pharmaceuticals, Inc.

  公开号：US20220409555A1

  公开（公告）日：2022-12-29

  Provided herein are arylcyclohexylanine derivatives and their use in the treatment of psychiatric disorders.
• [EN] ARYLCYCLOHEXYLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PSYCHIATRIC DISORDERS<br/>[FR] DÉRIVÉS ARYLCYCLOHEXYLAMINE ET LEUR UTILISATION DANS LE TRAITEMENT DE TROUBLES PSYCHIATRIQUES
  申请人：GILGAMESH PHARMACEUTICALS INC

  公开号：WO2021134086A1

  公开（公告）日：2021-07-01

  Provided herein are arylcyclohexylamine derivatives and their use in the treatment of psychiatric disorders.

  本文提供了芳基环己胺衍生物及其在治疗精神疾病中的用途。