Journal article
Silanetriols as in vitro AChE Inhibitors
Publication Details
Authors: | Blunder, M.; Hurkes, N.; Spirk, S.; List, M.; Pietschnig, R. |
Publisher: | Elsevier B. V. |
Publication year: | 2011 |
Journal: | Bioorganic and Medicinal Chemistry Letters |
Pages range : | 363-365 |
Volume number: | 21 |
Issue number: | 21 |
Start page: | 363 |
End page: | 365 |
ISSN: | 0960-894X |
DOI-Link der Erstveröffentlichung: |
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 concn. 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 μM was detd. as well. The cytotoxicity of the silanetriols used was negligible at concns. relevant for inhibition. [on SciFinder(R)]
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 concn. 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 μM was detd. as well. The cytotoxicity of the silanetriols used was negligible at concns. relevant for inhibition. [on SciFinder(R)]
Keywords
silanetriol steric protection acetylcholinesterase inhibitor
