Synthesis of 1,4-dihydro-2-phenyl-4,4-bis(4-pyridinylmethyl)-2H-isoquinolin-3-one and related compounds as acetylcholine release enhancers

Mei Shan Lin, Ling Wei Hsin, Hui Bing Tsai, Ming Cheng Tsai, Chen Yu Cheng

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Acetylcholine release enhancers may have therapeutic value in the treatment of Alzheimer's disease. A series of 1,4-dihydro-4,4-bis(pyridinylmethyl)-2H-isoquinolin-3-ones (2-13) was synthesized as analogs of the known acetylcholine-release enhancer linopirdine (1). Their cholinergic activity was measured as the enhancement of indirectly-elicited twitch tension of the mouse diaphragm. Among the target compounds, 2-phenyl-4,4-bis(4-pyridinylmethyl)-4H-isoquinoline-1,3-dione (2) and 7-bromo-1,4-dihydro-2-phenyl-4,4-bis(4-pyridinylmethyl)-2H-isoquinolin-3-one (11) were found to be more potent than 1.

Original languageEnglish
Pages (from-to)271-281
Number of pages11
JournalChinese Pharmaceutical Journal
Issue number4
Publication statusPublished - Aug 2002



  • Acetylcholine release enhancers
  • Alzheimer's disease
  • Linopirdine

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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