- Synthesis of antagonists of muscarinic (M3) receptors
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Several α-hydroxyamides with (2,6-dialkoxyphenoxy)methyl substituents have been prepared and their activities as antagonists of the M3 muscarinic receptor in guinea pig ileum have been evaluated. N-{1-[(Phenyl)methyl]piperidin-4-yl}-2-{2-[(2,6-dimethoxyphenoxy)-methyl]phenyl} -2-hydroxypropanamide and N-(1-[{6-amino-4-[(1-propylpiperidin-4-yl)methyl]- pyridin-2-yl}methyl]piperidin-4-yl)-2-cyclopentyl-2-hydroxy-2-phenylacetamide were the most potent compounds prepared, the micromolar potency of the latter indicating that it may be worth further investigation.
- Broadley, Kenneth J.,Davies, Robin H.,Escargueil, Christine,Lee, Alan T.L.,Penson, Peter,Thomas, Eric J.
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experimental part
p. 781 - 801
(2012/01/12)
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- NOVEL POTASSIUM CHANNEL BLOCKERS AND USES THEREOF
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The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevent
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- Preparation of chlorosyringols and chloropyrogallols - Components of pulp bleaching effluents
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The preparation and properties of chlorosyringols and chloropyrogallols, components of pulp bleaching effluents, and their acetates are given. The compounds are obtained mainly by direct chlorination of both phenols or of syringol acetate with various chlorinating reagents. 5-Chloropyrogallol and 4,5-dichloropyrogallol were the products of demethylation of 5-chloro-3-methoxycatechol acetate and 4,5-dichloro-3-methoxycatechol acetate, respectively. The acetates of all ten chloro compounds were separated by gas chromatography. Electron impact mass spectra and 1H and 13C NMR data for the acetates are given.
- Smith,Wearne,Wallis
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p. 921 - 930
(2007/10/03)
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