6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.

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Schott Y, Decker M, Rommelspacher H, Lehmann J

6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5840-3. Epub 2006 Sep 1.

PubMed ID
16945529 [ View in PubMed
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Abstract

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 beta-carbolines (BCs). 6-Oxygenated beta-carboline and beta-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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
GalantamineAcetylcholinesteraseIC 50 (nM)600N/AN/ADetails
PhysostigmineAcetylcholinesteraseIC 50 (nM)500N/AN/ADetails
RivastigmineAcetylcholinesteraseIC 50 (nM)48000N/AN/ADetails