Silanetriols as in vitro inhibitors for AChE

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 ste...

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Detalles Bibliográficos
Autores principales: Blunder, Martina, Hurkes, Natascha, Spirk, Stefan, List, Martina, Pietschnig, Rudolf
Formato: Texto
Lenguaje:English
Publicado: Elsevier Science Ltd 2011
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3013380/
https://www.ncbi.nlm.nih.gov/pubmed/21111617
http://dx.doi.org/10.1016/j.bmcl.2010.10.139
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author Blunder, Martina
Hurkes, Natascha
Spirk, Stefan
List, Martina
Pietschnig, Rudolf
author_facet Blunder, Martina
Hurkes, Natascha
Spirk, Stefan
List, Martina
Pietschnig, Rudolf
author_sort Blunder, Martina
collection PubMed
description 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.
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spelling pubmed-30133802011-02-11 Silanetriols as in vitro inhibitors for AChE Blunder, Martina Hurkes, Natascha Spirk, Stefan List, Martina Pietschnig, Rudolf Bioorg Med Chem Lett Article 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. Elsevier Science Ltd 2011-01-01 /pmc/articles/PMC3013380/ /pubmed/21111617 http://dx.doi.org/10.1016/j.bmcl.2010.10.139 Text en © 2011 Elsevier Ltd. https://creativecommons.org/licenses/by-nc-nd/3.0/ Open Access under CC BY-NC-ND 3.0 (https://creativecommons.org/licenses/by-nc-nd/3.0/) license
spellingShingle Article
Blunder, Martina
Hurkes, Natascha
Spirk, Stefan
List, Martina
Pietschnig, Rudolf
Silanetriols as in vitro inhibitors for AChE
title Silanetriols as in vitro inhibitors for AChE
title_full Silanetriols as in vitro inhibitors for AChE
title_fullStr Silanetriols as in vitro inhibitors for AChE
title_full_unstemmed Silanetriols as in vitro inhibitors for AChE
title_short Silanetriols as in vitro inhibitors for AChE
title_sort silanetriols as in vitro inhibitors for ache
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3013380/
https://www.ncbi.nlm.nih.gov/pubmed/21111617
http://dx.doi.org/10.1016/j.bmcl.2010.10.139
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