Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas

SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M3 over M1. The structure–activity relationships (SAR) and optimization of the tyrosine urea series are described.

SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good sub-type selectivity for M3 over M1. The structure–activity relationships (SAR) and optimization of the tyrosine urea series are described.Figure optionsDownload as PowerPoint slide