Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.

Jian Jin,Yonghui Wang,Dongchuan Shi,Feng Wang,Wei Fu,Roderick S Davis,Qi Jin,James J Foley,Henry M Sarau,Dwight M Morrow,Michael L Moore,Ralph A Rivero,Michael Palovich,Michael Salmon,Kristen E Belmonte,Jakob Busch-Petersen

Bioorganic & Medicinal Chemistry Letters（2008）

Cited 6|Views65

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Abstract

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.

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Key words

Muscarinic acetylcholine receptor antagonists,M3 mAChR,SAR,Subtype selectivity,COPD,Asthma,Tyrosine ureas

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