Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
Article Details
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Tumiatti V, Milelli A, Minarini A, Rosini M, Bolognesi ML, Micco M, Andrisano V, Bartolini M, Mancini F, Recanatini M, Cavalli A, Melchiorre C
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
J Med Chem. 2008 Nov 27;51(22):7308-12. doi: 10.1021/jm8009684.
- PubMed ID
- 18954037 [ View in PubMed]
- Abstract
Novel multi-target-directed ligands were designed by replacing the inner dipiperidino function of 3 with less flexible or completely rigid moieties to obtain compounds endowed with multiple biological properties that might be relevant to Alzheimer's disease. 15 was the most interesting, inhibiting AChE in the nanomolar range and inhibiting AChE-induced and self-promoted beta-amyloid aggregation in the micromolar range.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Donepezil Acetylcholinesterase IC 50 (nM) 23.1 N/A N/A Details Galantamine Acetylcholinesterase IC 50 (nM) 2010 N/A N/A Details