Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
Article Details
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Bolognesi ML, Andrisano V, Bartolini M, Banzi R, Melchiorre C
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
J Med Chem. 2005 Jan 13;48(1):24-7.
- PubMed ID
- 15633997 [ View in PubMed]
- Abstract
Heterodimers 4 and 5 were effective inhibitors of acetylcholinesterase (AChE) activity and AChE-induced amyloid-beta (A beta) aggregation. The peculiar biological profile of 4 can be relevant in studying the molecular basis underlying the nonclassical action of AChE and in addressing the question whether AChE inhibitors can affect the neurotoxic cascade leading to Alzheimer's disease. Compound 4 emerged as the most potent heterodimer so far available to inhibit AChE-induced A beta aggregation.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Tacrine Acetylcholinesterase Ki (nM) 151 N/A N/A Details Tacrine Acetylcholinesterase IC 50 (nM) 424 N/A N/A Details