2′ Biaryl amides as novel and subtype selective M 1 agonists. Part I: Identification, synthesis, and initial SAR

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

Index: Budzik, Brian; Garzya, Vincenzo; Shi, Dongchuan; Foley, James 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. 3540 - 3544

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Citation Number: 12

Abstract

Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure–activity relationships that led to compounds 3j and 4c, possessing good M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2–5, are described.