Synthesis and Structure-Activity Relationships of N-Propyl-N-(4-pyridinyl)-1 H-indol-1-amine (Besipirdine) and Related Analogs as Potential Therapeutic Agents for …

…, RD Blitzer, E Landau, V Haroutunian…

文献索引：Klein; Davis; Olsen; Wong; Huger; Smith; Petko; Cornfeldt; Wilker; Blitzer; Landau; Haroutunian; Martin; Effland Journal of Medicinal Chemistry, 1996 , vol. 39, # 2 p. 570 - 581

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被引用次数: 32

摘要

A series of novel N-(4-pyridinyl)-1 H-indol-1-amines and other heteroaryl analogs was synthesized and evaluated in tests to determine potential utility for the treatment of Alzheimer's disease. From these compounds, N-propyl-N-(4-pyridinyl)-1 H-indol-1-amine (besipirdine, 4c) was selected for clinical development based on in-depth biological evaluation. In addition to cholinomimetic properties based initially on in vitro inhibition of [ ...