2-phenyl-11-(2-N,N-dimethylaminoethyl)isoindolo[2,1-a]indol-6-one | 1375501-08-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-phenyl-11-(2-N,N-dimethylaminoethyl)isoindolo[2,1-a]indol-6-one
• CAS: 1375501-08-8
• 化学式: C₂₅H₂₂N₂O
• 分子量: 366.462
• InChiKey: FXJWLPCPEQZGLQ-UHFFFAOYSA-N

反应信息

• 作为产物：
  描述：

  在 四(三苯基膦)钯 、 potassium acetate 作用下， 以 N,N-二甲基乙酰胺 为溶剂， 反应 5.0h， 以56.1%的产率得到2-phenyl-11-(2-N,N-dimethylaminoethyl)isoindolo[2,1-a]indol-6-one
  参考文献：
  名称：

  Synthesis and structure–activity relationship of novel conformationally restricted analogues of serotonin as 5-HT₆ receptor ligands

  摘要：

  5-Hydroxytryptamine 6 receptors (5-HT6R) are being perceived as the possible target for treatment of cognitive disorders as well as obesity. The present article deals with the design, synthesis, in vitro binding and structure-activity relationship of a novel series of tetracyclic tryptamines with the rigidized N-arylsulphonyl, N-arylcarbonyl and N-benzyl substituents as 5-HT6 receptor ligands. The chiral sulphonyl derivatives 15a and 17a showed high affinity at 5-HT6R with the K-i of 23.4 and 20.5 nM, respectively. The lead compound from the series 15a has acceptable ADME properties, adequate brain penetration and is active in animal models of cognition like Novel Object Recognition Task (NORT) and water maze.

  DOI：

  10.3109/14756366.2011.595713