C-(4-氟-联苯-4-基)-甲胺盐酸盐 | 518357-40-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: C-(4-氟-联苯-4-基)-甲胺盐酸盐
• 中文别名: [4-（4-氟苯基）苯基]甲胺盐酸盐
• 英文名称: (4′-fluorobiphenyl-4-yl)methylammonium chloride
• 英文别名: (4'-fluorobiphenyl-4-yl)methylamine hydrochloride；[4-(4-Fluorophenyl)phenyl]methylamine hydrochloride；[4-(4-fluorophenyl)phenyl]methanamine;hydrochloride
• CAS: 518357-40-9
• 化学式: C₁₃H₁₂FN*ClH
• 分子量: 237.704
• InChiKey: IZUWYHXAARRMGW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.37
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  26
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  C-(4-氟-联苯-4-基)-甲胺盐酸盐 在 sodium hydroxide 作用下， 以 水 为溶剂， 生成 (4’-氟联苯-4-基)甲胺
  参考文献：
  名称：

  Substituted N-(Biphenyl-4′-yl)methyl (R)-2-Acetamido-3-methoxypropionamides: Potent Anticonvulsants That Affect Frequency (Use) Dependence and Slow Inactivation of Sodium Channels

  摘要：

  We prepared 13 derivatives of N-(biphenyl-4'-yl)methyl (R)-2-acetamido-3-methoxypropionamide that differed in type and placement of a R-substituent in the terminal aryl unit. We demonstrated that the R-substituent impacted the compound's whole animal and cellular pharmacological activities. In rodents, select compounds exhibited excellent anticonvulsant activities and protective indices (PI = TD50/ED50) that compared favorably with clinical antiseizure drugs. Compounds with a polar, aprotic R-substituent potently promoted Na+ channel slow inactivation and displayed frequency (use) inhibition of Na+ currents at low micromolar concentrations. The possible advantage of affecting these two pathways to decrease neurological hyperexcitability is discussed.

  DOI：

  10.1021/jm500707r
• 作为产物：
  描述：

  (4’-氟联苯-4-基)甲胺 在 盐酸 作用下， 以 水 、 乙酸乙酯 为溶剂， 反应 1.0h， 以4.99 g的产率得到C-(4-氟-联苯-4-基)-甲胺盐酸盐
  参考文献：
  名称：

  (Biphenyl-4-yl)methylammonium Chlorides: Potent Anticonvulsants That Modulate Na⁺ Currents

  摘要：

  We have reported that compounds containing a biaryl linked unit (Ar-X-Ar') modulated Na+ currents by promoting slow inactivation and fast inactivation processes and by inducing frequency (use)-dependent inhibition of Na+ currents. These electrophysiological properties have been drugs. In this study, we demonstrate that the readily accessible associated with the mode of action of several antiepileptic (biphenyl-4-yl)methylammonium chlorides (compound class B) exhibited a broad range of anticonvulsant activities in animal models, and in the maximal electroshock seizure test the activity of (3'-trifluoromethoxybiphenyl-4-yl)methylammonium chloride (8) exceeded that of phenobarbital and phenytoin upon oral administration to rats. Electrophysiological studies of 8 using mouse catecholamine A-differentiated cells and rat embryonic cortical neurons confirmed that 8 promoted slow and fast inactivation in both cell types but did not affect the frequency (use)-dependent block of Na+ currents.

  DOI：

  10.1021/jm4007092

文献信息

• Hepatitis B core protein modulators
  申请人：Assembly Biosciences, Inc.

  公开号：US10766890B2

  公开（公告）日：2020-09-08

  The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.

  本公开内容部分提供了对乙型肝炎病毒 Cp 具有异生效应特性的化合物。本文还提供了治疗病毒感染（如乙型肝炎）的方法，包括向有需要的患者施用所公开的化合物。
• HEPATITIS B CORE PROTEIN MODULATORS
  申请人：Assembly Biosciences, Inc.

  公开号：EP3349581B1

  公开（公告）日：2021-12-01