Structure-activity studies on acetylcholinesterase inhibition in the lycorine series of Amaryllidaceae alkaloids.

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McNulty J, Nair JJ, Little JR, Brennan JD, Bastida J

Structure-activity studies on acetylcholinesterase inhibition in the lycorine series of Amaryllidaceae alkaloids.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5290-4. doi: 10.1016/j.bmcl.2010.06.130. Epub 2010 Jul 1.

PubMed ID

20655219 [ View in PubMed

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Abstract

The synthesis of differentially functionalized analogs of the Amaryllidaceae alkaloid lycorine, accessed via a concise chemoselective silylation strategy, is described uncovering two of the most potent inhibitors of acetylcholinesterase (AChE) identified to date in this series. Important elements of this novel pharmacophore were elucidated through structure-activity relationship (SAR) studies.

DrugBank Data that Cites this Article

Binding Properties

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