Silanetriols as in vitro inhibitors for AChE

Martina Blunder; Natascha Hurkes; Stefan Spirk; Martina List; Rudolf Pietschnig

doi:10.1016/j.bmcl.2010.10.139

Silanetriols as in vitro inhibitors for AChE

Bioorg Med Chem Lett. 2011 Jan 1;21(1):363-5. doi: 10.1016/j.bmcl.2010.10.139. Epub 2010 Nov 5.

Authors

Martina Blunder¹, Natascha Hurkes, Stefan Spirk, Martina List, Rudolf Pietschnig

Affiliation

¹ Institut für Chemie, Karl-Franzens-Universität Graz, Schubertstrasse 1, 8010 Graz, Austria.

Abstract

Three stable silanetriols with increasing steric protection of the silicon atom have been tested for inhibition of acetylcholinesterase (AChE). For all tested silanetriols we found reversible inhibition of the AChE activity at a 100 μM concentration. The highest inhibition rate was found for the sterically least hindered cyclohexylsilanetriol with 45% inhibition relative to galanthamine hydrobromide for which an IC(50) value of 121 ± 3 μM was determined as well. The cytotoxicity of the silanetriols used was found to be negligible at concentrations relevant for inhibition.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acetylcholinesterase / chemistry*
Acetylcholinesterase / metabolism
Cell Line
Cholinesterase Inhibitors / chemical synthesis
Cholinesterase Inhibitors / chemistry*
Cholinesterase Inhibitors / toxicity
Humans
Organosilicon Compounds / chemistry*
Organosilicon Compounds / toxicity
Silanes / chemistry*

Substances

Cholinesterase Inhibitors
Organosilicon Compounds
Silanes
silanol
Acetylcholinesterase