Synthesis of antagonists of muscarinic (M3) receptors

Broadley, Kenneth John ORCID: https://orcid.org/0000-0002-3339-2050, Davies, Robin H., Escargueil, Christine, Lee, Alan T. L., Penson, Peter Edward and Thomas, Eric J. 2011. Synthesis of antagonists of muscarinic (M3) receptors. Collection Of Czechoslovak Chemical Communications 76 (7) , pp. 781-801. 10.1135/cccc2011017

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Abstract

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.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Pharmacy
Subjects:	R Medicine > RM Therapeutics. Pharmacology R Medicine > RS Pharmacy and materia medica
Uncontrolled Keywords:	Muscarinic receptors; Antagonists; Suzuki–Miyaura coupling; α-Hydroxyamides; Alcohols; Amides; Biological activity; Medicinal chemistry
Additional Information:	Effective January 1, 2012, the journal is published under the name ChemPlusChem by Wiley-VCH.
Publisher:	Institute of Organic Chemistry and Biochemistry
ISSN:	0010-0765
Related URLs:	http://dx.doi.org/10.1002/chin.201143140
Last Modified:	18 Oct 2022 13:47
URI:	https://orca.cardiff.ac.uk/id/eprint/15436

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