2′ Biaryl amides as novel and subtype selective M 1 agonists. Part II: Further optimization and profiling

…, CJ Langmead, J Watson, Z Wu, IT Forbes, J Jin

Index: Budzik, Brian; Garzya, Vincenzo; Shi, Dongchuan; Walker, Graham; Lauchart, Yann; Lucas, Adam J.; Rivero, Ralph A.; Langmead, Christopher J.; Watson, Jeannette; Wu, Zining; Forbes, Ian T.; Jin, Jian Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 12 p. 3545 - 3549

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Citation Number: 14

Abstract

Further optimization of the biaryl amide series via extensively exploring structure–activity relationships resulted in potent and subtype selective M1 agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure–activity relationships, subtype selectivity for M1 over M2–5, and DMPK properties of these novel compounds are described.