| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367324 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
In the course of studies directed toward the discovery of novel acetyl- and butyrylcholinesterase (AChE and BChE) inhibitors for the treatment of Alzheimer‘s disease, we focused on β-carbolines (BCs). 6-Oxygenated β-carboline and β-carbolinium derivatives based on the serotonin template were synthesized and tested in vitro for their ability to inhibit AChE and BChE, respectively. Particularly the carbolinium salts, which can be formed by intracerebral methylation out of the tertiary-BC prodrugs, show inhibitory activity levels reaching those of galantamine, physostigmine, and rivastigmine.
Graphical abstractA series of β-carbolines and β-carbolinium salts were synthesized and their inhibitory activities towards AChE and BChE measured. Micromolar inhibitors with some selectivity toward AChE were identified.Figure optionsDownload full-size imageDownload as PowerPoint slide
