2′ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR

Biaryl amides were discovered as novel and subtype selective M1 agonists. The identification, synthesis, and initial SAR that led to the discovery of compound 3j are described. Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identificat...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-06, Vol.20 (12), p.3540-3544
Hauptverfasser: Budzik, Brian, Garzya, Vincenzo, Shi, Dongchuan, Foley, James J., Rivero, Ralph A., Langmead, Christopher J., Watson, Jeannette, Wu, Zining, Forbes, Ian T., Jin, Jian
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Sprache:eng
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Zusammenfassung:Biaryl amides were discovered as novel and subtype selective M1 agonists. The identification, synthesis, and initial SAR that led to the discovery of compound 3j are described. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.04.128