N-2-(2-methoxy-4-pyridyl)ethylpropanamide | 170026-11-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-2-(2-methoxy-4-pyridyl)ethylpropanamide
• 英文别名: N-[2-(2-methoxypyridin-4-yl)ethyl]propanamide
• CAS: 170026-11-6
• 化学式: C₁₁H₁₆N₂O₂
• 分子量: 208.26
• InChiKey: JWMPVZCVQFEIDU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  51.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-2-(2-methoxy-4-pyridyl)ethylpropanamide 在 sodium tetrahydroborate 、 lithium aluminium tetrahydride 、 溶剂黄146 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 60.0h， 生成 N,N-di-n-propyl-2-(2-methoxy-4-pyridyl)ethylamine
  参考文献：
  名称：

  New 2-pyridylethylamines with dopaminergic activity: Synthesis and radioligand-binding evaluation

  摘要：

  In order to determine whether the pyridine nucleus could replace the catechol moiety of the neurotransmitter dopamine or the phenol ring of the dopaminergic pharmacophore m-hydroxyphenylethylamine, the 2-(3-pyridyl)ethylamine 7, 2-(4-pyridyl)ethylamine 8, 2-(2-hydroxy-4-pyridyl) ethylamine 10 and their N,N-di-n-propyl- and N-n-propyl-N-2-phenylethyl derivatives were synthesized. The affinities of the new compounds for D-1 and D-2 dopamine receptors were evaluated by displacement of [H-3]SCH 23390 (D-1 selective) and [H-3]spiperone (D-2 selective) on rat neostriatum sections. The 2-(4-pyridyl)ethylamine 8 and its N,N-di-n-propyl derivative 18 showed the same affinity for the D-1 and D-2 receptors. Other compounds bound to the D-1 receptor with higher affinity than to the D-2 receptor. The possibility that the above compounds act as agonists and antagonists at the dopamine D-1 and D-2 receptors is discussed on the basis of guanosine-5'-triphosphate and Na+ displacement curves.

  DOI：

  10.1016/0223-5234(96)88251-1
• 作为产物：
  描述：

  2-甲氧基-4-吡啶丙酸 在 sodium azide 、 硫酸 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 26.0h， 生成 N-2-(2-methoxy-4-pyridyl)ethylpropanamide
  参考文献：
  名称：

  New 2-pyridylethylamines with dopaminergic activity: Synthesis and radioligand-binding evaluation

  摘要：

  In order to determine whether the pyridine nucleus could replace the catechol moiety of the neurotransmitter dopamine or the phenol ring of the dopaminergic pharmacophore m-hydroxyphenylethylamine, the 2-(3-pyridyl)ethylamine 7, 2-(4-pyridyl)ethylamine 8, 2-(2-hydroxy-4-pyridyl) ethylamine 10 and their N,N-di-n-propyl- and N-n-propyl-N-2-phenylethyl derivatives were synthesized. The affinities of the new compounds for D-1 and D-2 dopamine receptors were evaluated by displacement of [H-3]SCH 23390 (D-1 selective) and [H-3]spiperone (D-2 selective) on rat neostriatum sections. The 2-(4-pyridyl)ethylamine 8 and its N,N-di-n-propyl derivative 18 showed the same affinity for the D-1 and D-2 receptors. Other compounds bound to the D-1 receptor with higher affinity than to the D-2 receptor. The possibility that the above compounds act as agonists and antagonists at the dopamine D-1 and D-2 receptors is discussed on the basis of guanosine-5'-triphosphate and Na+ displacement curves.

  DOI：

  10.1016/0223-5234(96)88251-1

文献信息

• COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE
  申请人：SHY Therapeutics LLC

  公开号：US20170174699A1

  公开（公告）日：2017-06-22

  Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

  本文提供了抑制MAPK磷酸化的化合物，因此可用于治疗癌症和炎症性疾病的组合物和方法。
• [EN] COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DU CANCER ET DE MALADIES INFLAMMATOIRES
  申请人：SHY THERAPEUTICS LLC

  公开号：WO2017112777A1

  公开（公告）日：2017-06-29

  Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are compositions and methods for treating cancer and inflammatory disease.