A novel series of tacrine–selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease

A novel series of tacrine–selegiline hybrids was synthesised and evaluated for application as inhibitors of cholinesterase (AChE/BuChE) and monoamine oxidase (MAO-A/B). The results demonstrate that most of the synthesised compounds exhibit high inhibitory activity. Among these compounds, compound 8g provided a good balance of activity towards all targets (with IC50 values of 22.6 nM, 9.37 nM, 0.3724 μM, and 0.1810 μM for AChE, BuChE, MAO-A and MAO-B, respectively). These results indicated that 8g has the potential to be a multi-functional candidate for Alzheimer's disease.

Figure optionsDownload as PowerPoint slideHighlights
► Thirteen tacrine–selegiline hybrids, as anti-Alzheimer agents were synthesised.
► Most of the compounds showed high inhibitory activities for AChE and BuChE.
► Most of the compounds showed good inhibitory activities for MAO-A and MAO-B.