Aufsatz in einer Fachzeitschrift
Silanetriols as in vitro AChE Inhibitors
Details zur Publikation
Autor(inn)en: | Blunder, M.; Hurkes, N.; Spirk, S.; List, M.; Pietschnig, R. |
Verlag: | Elsevier B. V. |
Publikationsjahr: | 2011 |
Zeitschrift: | Bioorganic and Medicinal Chemistry Letters |
Seitenbereich: | 363-365 |
Jahrgang/Band : | 21 |
Heftnummer: | 21 |
Erste Seite: | 363 |
Letzte Seite: | 365 |
ISSN: | 0960-894X |
DOI-Link der Erstveröffentlichung: |
Zusammenfassung, 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)]
Schlagwörter
silanetriol steric protection acetylcholinesterase inhibitor
