A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.
Article Details
- CitationCopy to clipboard
Lu C, Zhou Q, Yan J, Du Z, Huang L, Li X
A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.
Eur J Med Chem. 2013 Apr;62:745-53. doi: 10.1016/j.ejmech.2013.01.039. Epub 2013 Feb 8.
- PubMed ID
- 23454517 [ View in PubMed]
- Abstract
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 muM, and 0.1810 muM 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Clorgiline Amine oxidase [flavin-containing] A IC 50 (nM) 4.1 N/A N/A Details Pargyline Amine oxidase [flavin-containing] B IC 50 (nM) 188 N/A N/A Details