SYNTHESIS OF ANTAGONISTS OF MUSCARINIC (M3) RECEPTORS

被引：2

作者：

Broadley, Kenneth J. ^{[3
]}

Davies, Robin H. ^{[2
]}

Escargueil, Christine ^{[3
]}

Lee, Alan T. L. ^{[1
]}

Penson, Peter ^{[3
]}

Thomas, Eric J. ^{[1
]}

机构：

[1] Univ Manchester, Sch Chem, Manchester M13 9PL, Lancs, England

[2] Muscagen Ltd, Cardiff CF10 3DFY, S Glam, Wales

[3] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3NB, S Glam, Wales

来源：

COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS | 2011年 / 76卷 / 07期

关键词：

Muscarinic receptors; Antagonists; Suzuki-Miyaura coupling; alpha-Hydroxyamides; Alcohols; Amides; Biological activity; Medicinal chemistry; HIGH SELECTIVITY; OXIDATION; ALDEHYDES; ALCOHOLS;

D O I：

10.1135/cccc2011017

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Several alpha-hydroxyamides with (2,6-dialkoxyphenoxy) methyl substituents have been prepared and their activities as antagonists of the M-3 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.

引用

页码：781 / 801

页数：21

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