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Synthesis of antagonists of muscarinic (M3) receptors

Broadley, Kenneth John ORCID:, 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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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:
Last Modified: 18 Oct 2022 13:47

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