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- (Hydroxymethyl)diphenyl(piperidinoalkyl)silanes (1)
- 1,4-Dioxa-2 (1)
- 5-disila-cyclohexane ring system (1)
- Sila-difenidol (1)
- Sila-pridinol (1)
- X-ray (1)
- antimuscarinic and papaverine-like activity (1)
- conformational anaylses (1)
- crystal and molecular structure (1)
- curare-lik activity (1)
- muscarinic antagonists (1)
- muscarinic receptors (1)
- sila-substitution (1)
- silicon compounds (1)
- structure (1)
- structure-activity relationships (1)
- synthesis (1)
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No abstract available.
The 2,2,5,5-tetraorganyl-1,4-dioxa-2,5-disilacyclohexanes 2a-2c were prepared by condensation of the corresponding (hydroxymethyl)diorganylsilanes 1 a-1 c. The constitution of the heterocycles was confirmed by elemental analyses, cryoscopic measurements, mass spectrometry, and NMR-spectroscopic \((^1H, ^{13}C)\) investigations. The molecular structure of 2 b was determined by X-ray diffraction analysis.
In the course of systematic investigations on sila-substituted parasympatholytics the diphenyl(2-aminoethoxymethyl)silanols 3b and 4b (and its carbon analogue 4a) were synthesized and characterized by their physical and chemical properties. In the solid state 4a and 4b form strong O-H---N hydrogen bonds, which are intramolecular (4a) and intermolecular (4b), respectively. 4a and 4b were found to be weak antimuscarinic agents (4b >4a) and strong papaverine-like spasmolytics (4a ≈4b).
The potentially curare-like silicon compounds 8a- 8f were synthesized and investigated with respect to their structure-activity relationships. The conformations of the compounds in the solid state and in solution were studied by X-ray diffraction analysis (8a- 8e) and IR NMR spectroscopy (8a- 8f), respectively. The muscle relaxing properties of 8a- 8f were investigated on the mouse. The observed structure-activity relationships are not in accordance with the classical "14 Å model" for neuromuscular blocking agents.