Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.

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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
DrugTargetPropertyMeasurementpHTemperature (°C)
DonepezilAcetylcholinesteraseIC 50 (nM)23.1N/AN/ADetails
GalantamineAcetylcholinesteraseIC 50 (nM)2010N/AN/ADetails