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

Exploration of multiple regions of a bi-aryl amine template led to the identification of highly potent M3 muscarinic acetylcholine receptor antagonists such as 14 (pA2 = 11.0) possessing good sub-type selectivity for M3 over M2. The structure–activity relationships (SAR) and optimization of the bi-aryl amine series are described.

Exploration of multiple regions of a bi-aryl amine template led to the identification of highly potent M3 muscarinic acetylcholine receptor antagonists such as 14 possessing good sub-type selectivity for M3 over M2. The structure–activity relationships and optimization of the bi-aryl amine series are described.Figure optionsDownload as PowerPoint slide