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

Brian Budzik,Yonghui Wang,Dongchuan Shi,Feng Wang,Haibo Xie,Zehong Wan,Chongye Zhu,James J Foley,Parvathi Nuthulaganti,Lorena A Kallal,Henry M Sarau,Dwight M Morrow,Michael L Moore,Ralph A Rivero,Michael Palovich,Michael Salmon,Kristen E Belmonte,Dramane I Laine,Jian Jin

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

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.

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关键词

Muscarinic acetylcholine receptor,M3 mAChR,Antagonists,SAR,Sub-type selectivity,COPD,Asthma,Bi-aryl amines

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