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Synthesis of antagonists of muscarinic (M3) receptors

Broadley, Kenneth John, 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: 05 Jan 2018 20:57

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