Synthesis and Anticholinesterase Evaluation of Cassine, Spectaline and Analogues

In this work, twelve analogues of piperidine alkaloids (-)-cassine and (-)-spectaline were synthesized, as well the racemic forms these natural products. The compounds evaluated for their inhibition electric eel acetylcholinesterase (AChEee) human butyrylcholinesterase (BChEhu) by on-flow mass-spectrometry-based dual-enzyme assay, mechanisms most potent also determined. Our results showed a preference BChEhu with 10c (Ki = 5.24 ?M), 12b 17.4 13a 13.2 ?M) 3 11.3 displaying best inhibitory activities.