Prospective acetylcholinesterase inhibitory activity of indole and its analogs.

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Khorana N, Changwichit K, Ingkaninan K, Utsintong M

Prospective acetylcholinesterase inhibitory activity of indole and its analogs.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2885-8. doi: 10.1016/j.bmcl.2012.02.057. Epub 2012 Feb 27.

PubMed ID

22425563 [ View in PubMed

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Abstract

Acetylcholinesterase (AChE) inhibitory activity is one of the proposed targets for indole analogs. Simple indoles with substitution of methoxy, carboxy or hydroxy at the benzene ring showed a low percent of inhibitory activity in eel-AChE. Adding a side chain at the pyrrole ring, such as serotonin, beta-carbolines and quinolines (the bioisostere of indole), improved the inhibitory activity significantly. However, proper substitution and conformation of the ring were required for good binding. The result of inhibition in human-AChE of serotonin, beta-carbolines and quinolines showed similar profile as eel-AChE with lower magnitude. The data from molecular docking showed that they shared the same binding site as galantamine.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Galantamine	Acetylcholinesterase	IC 50 (nM)	300	N/A	N/A	Details