Silanetriols as in vitro inhibitors for AChE

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Blunder, Martina¹  Hurkes, Natascha¹  Spirk, Stefan¹  List, Martina¹  Pietschnig, Rudolf¹ 

[1] Karl Franzens Univ Graz, Inst Chem, A-8010 Graz, Austria

关键词: Inhibition;    Model compound;    Transition state;    Silanol;    Toxicity;    Silicone;   

DOI  :  10.1016/j.bmcl.2010.10.139

来源: Elsevier

【 摘 要 】

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 mu M concentration. The highest inhibition rate was found for the sterically least hindered cyclohexylsilanetriol with 45% inhibition relative to galanthamine hydrobromide for which an IC50 value of 121 +/- 3 mu M was determined as well. The cytotoxicity of the silanetriols used was found to be negligible at concentrations relevant for inhibition. (C) 2010 Elsevier Ltd. All rights reserved.

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