(E)-N1-(naphthalen-1-yl)ethene-1,2-diamine | 1044903-79-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: (E)-N1-(naphthalen-1-yl)ethene-1,2-diamine
• 英文别名: (E)-N'-naphthalen-1-ylethene-1,2-diamine
• CAS: 1044903-79-8
• 化学式: C₁₂H₁₂N₂
• 分子量: 184.241
• InChiKey: ZDPNQLMJTIMGGN-CMDGGOBGSA-N

物化性质

• 沸点：
  349.2±34.0 °C(Predicted)
• 密度：
  1.174±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (E)-methyl 3-(7-methoxy-4-oxo-4H-chromen-3-yl)acrylate 、 (E)-N1-(naphthalen-1-yl)ethene-1,2-diamine 在 三乙胺 作用下， 以 甲醇 为溶剂， 反应 8.0h， 以88%的产率得到(E)-5-(2-hydroxy-4-methoxybenzoyl)-1-(2-(naphthalen-1-ylamino)vinyl)pyridin-2(1H)-one
  参考文献：
  名称：

  Design, Synthesis, and Antihepatitis B Virus Activities of Novel 2-Pyridone Derivatives

  摘要：

  A series of novel 2-pyridone derivatives were synthesized and evaluated for their antihepatitis B virus (HBV) activity and cytotoxicity in vitro. Moderate to good activity against HBV DNA replication was observed in these 2-pyridone analogues. The most active compounds were 5d and 61, with good inhibitory activity against HBV DNA replication (IC50 = 0.206 and 0.12 mu M, respectively) and remarkable high selectivity (selectivity indexes of >532 and 467, respectively). A pharmacophore model of the synthesized compounds was proposed by the GASP program. The pharmacophore model consists of three hydrophobic points, four HBA points, and one HBD point. The 2-pyridone derivatives represent a novel class of HBV inhibitors, which are worth further optimization.

  DOI：

  10.1021/jm901237x

文献信息

• Compositions and methods for inhibiting arginase activity
  申请人：The Trustees of the University of Pennsylvania

  公开号：US20030036529A1

  公开（公告）日：2003-02-20

  Compositions and methods for inhibiting arginase activity, including arginase activity in a mammal, are provided. Methods of making the compositions of the invention are also provided as are methods of using the compositions therapeutically. The compositions described herein are useful for alleviating or inhibiting a variety of arinase- and NO synthase-related disorders, including heart diseae, gastrointestinal motility disorders, and penile erectile dysfunction in humans.

  本发明提供了抑制精氨酸酶活性的组合物和方法，包括哺乳动物中的精氨酸酶活性。本发明还提供了制备所述组合物的方法，以及使用所述组合物进行治疗的方法。所述组合物可用于缓解或抑制多种与精氨酸酶和NO合酶相关的疾病，包括心脏病、胃肠动力障碍和人类勃起功能障碍。
• Compositions for inhibiting arginase activity
  申请人：——

  公开号：US20040063666A1

  公开（公告）日：2004-04-01

  Compositions and methods for inhibiting arginase activity, including arginase activity in a mammal, are provided. Methods of making the compositions of the invention are also provided as are methods of using the compositions therapeutically. The compositions described herein are useful for alleviating or inhibiting a variety of arinase- and NO synthase-related disorders, including heart diseae, gastrointestinal motility disorders, and penile erectile dysfunction in humans.

  本发明提供了抑制精氨酸酶活性（包括哺乳动物体内的精氨酸酶活性）的组合物和方法。还提供了制造本发明组合物的方法以及治疗性使用组合物的方法。本文所述的组合物可用于缓解或抑制各种与精氨酸酶和 NO 合成酶相关的疾病，包括心脏病、胃肠道运动障碍和人类阴茎勃起功能障碍。
• US6387890B1
  申请人：——

  公开号：US6387890B1

  公开（公告）日：2002-05-14
• US6723710B2
  申请人：——

  公开号：US6723710B2

  公开（公告）日：2004-04-20