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Synthesis of antagonists of muscarinic (M3) receptors
Kenneth J. Broadley, Robin H. Davies, Christine Escargueil, Alan T. L. Lee, Peter Penson and Eric J. Thomas
Jazyk angličtina Země Česko Médium elektronický zdroj
NLK
ProQuest Central
od 2005-01-01 do 2011
- MeSH
- agonisté muskarinových receptorů MeSH
- antagonisté muskarinových receptorů MeSH
- biologické jevy MeSH
- klinická chemie MeSH
- morčata MeSH
- Check Tag
- morčata MeSH
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.
Muscagen Limited 10 North Road Cardiff CF10 3DFY UK
School of Chemistry University of Manchester M13 9PL UK
The Welsh School of Pharmacy Cardiff University King Edward 7 Avenue Cardiff CF10 3NB UK
Synthesis of antagonists of muscarinic (M3) receptors [elektronický zdroj] /
Literatura
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- $a 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.
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