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Bioorg Med Chem Lett. 2009 Mar 15;19(6):1686-90. doi: 10.1016/j.bmcl.2009.01.098. Epub 2009 Feb 4.

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

Author information

1
Centers of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA.

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.

PMID:
19243945
DOI:
10.1016/j.bmcl.2009.01.098
[Indexed for MEDLINE]

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