Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1394344 | European Journal of Medicinal Chemistry | 2013 | 9 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload 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.