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
收藏
页码：781 / 801
页数：21
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