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M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines

descriptionPublicationkeyboard_double_arrow_right Article 01 Mar 2009 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 19, pages 1,686-1,690 (issn: 0960-894X,

Authors: Ralph A. Rivero; Yonghui Wang; Henry M. Sarau; Michael Salmon; Zehong Wan; Chongye Zhu; Feng Wang; +12 Authors

doi: 10.1016/j.bmcl.2009.01.098

pmid: 19243945

M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines

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Abstract

Exploration of multiple regions of a bi-aryl amine template led to the identification of highly potent M(3) muscarinic acetylcholine receptor antagonists such as 14 (pA(2)=11.0) possessing good sub-type selectivity for M(3) over M(2). The structure-activity relationships (SAR) and optimization of the bi-aryl amine series are described.

Related Organizations

Cellzome, GSK, Middlesex, UK.
GlaxoSmithKline (United States)
United States

Keywords

Receptor, Muscarinic M3, Molecular Structure, Chemistry, Pharmaceutical, Electrons, Amides, Asthma, Inhibitory Concentration 50, Kinetics, Pulmonary Disease, Chronic Obstructive, Structure-Activity Relationship, Models, Chemical, Drug Design, Humans, Amines

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