Silanetriols as in vitro inhibitors for AChE

AbstractThree 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 100μM 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±3μM was determined as well. The cytotoxicity of the silanetriols used was found to be negligible at concentrations relevant for inhibition

Amphiphile Verbindungen der 14. Gruppe - Synthese, Eigenschaften und Anwendungen von Organosilanolen

FreChe Materie, Surfuncell Project, FWF, Land Steiermar

Silanetriols as Powerful Starting Materials for Selective Condensation to Bulky POSS Cages

Controlled condensation reactions of tertiary silanetriols CH₃(CH₂)_<i>n</i>(CH₃)₂CSi­(OH)₃ (<b>1b</b>–<b>f</b>; <i>n</i> = 1–5) in the presence of trifluoroacetic acid and the hydrolysis of CH₃(CH₂)₆(CH₃)₂CSiCl₃ (<b>3</b>) lead to the selective formation of the corresponding disiloxane tetrols [CH₃(CH₂)_<i>n</i>(CH₃)₂CSi­(OH)₂]₂O (<b>2b</b>–<b>g</b>; <i>n</i> = 1–6) in good yields. The TBAF-driven condensation reactions of the silanetriols CH₃(CH₂)_<i>n</i>(CH₃)₂CSi­(OH)₃ (<b>1a</b>–<b>c</b>; <i>n</i> = 0–2) as well as of the disiloxane-1,1,3,3-tetrol <b>2d</b> (<i>n</i> = 3) yield in the selective formation of the first T₈ cages bearing tertiary carbon substituents, CH₃(CH₂)_<i>n</i>(CH₃)₂C (<b>4a</b>–<b>d</b>; <i>n</i> = 0–3), which was not possible via the condensation of their alkoxysilane counterparts so far. The resulting compounds <b>2b</b>–<b>g</b> and <b>4a</b>–<b>d</b> have been characterized by multinuclear NMR, MS, and single-crystal X-ray diffraction