The discovery of VU0486846: steep SAR from a series of M PAMs based on a novel benzomorpholine core.

Jeanette L Bertron,Hyekyung P Cho,Pedro M Garcia-Barrantes,Joseph D Panarese,James M Salovich,Kellie D Nance,Darren W Engers,Jerri M Rook,Anna L Blobaum,Colleen M Niswender,Shaun R Stauffer,P Jeffrey Conn,Craig W Lindsley

Bioorganic & Medicinal Chemistry Letters（2018）

引用 9|浏览29

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摘要

•Detailed SAR leading to an M1 PAM devoid of cholinergic liability.•Enhanced sp3 character and enantiospecific M1 PAM activity.•Unexpected SAR form the fluorine walk strategy.

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关键词

M1,Muscarinic acetylcholine receptor,Positive allosteric modulator (PAM),Schizophrenia,Structure-Activity Relationship (SAR)

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