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 …
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 [ ...