2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.

Brian W Budzik,Vincenzo Garzya,Dongchuan Shi,Graham C Walker,Yann Lauchart,Adam J Lucas,Ralph A Rivero,Christopher J Langmead,Jeannette M Watson,Zining Wu,Ian Thomson Forbes,Jian Jin

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

Optimization and further SAR exploration of the biaryl amide series resulted in the discovery of orally bioavailable, CNS-penetrant M1 agonists with excellent potency and subtype selectivity.

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关键词

Subtype selective M1 muscarinic acetylcholine receptor agonist,Subtype selective M1 agonist,CNS-penetrant and orally bioavailable M1 agonist,2′ biaryl amides

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