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 M(1) muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M(1) agonist potency and intrinsic activity, and subtype selectivity for M(1) over M(2-5), are described.
Budzik
Brian
B
Discovery Research and Centers of Excellence for Drug Discovery, GlaxoSmithKline, Collegeville, PA 19426, USA. torqux@yahoo.com
Garzya
Vincenzo
V
Shi
Dongchuan
D
Foley
James J
JJ
Rivero
Ralph A
RA
Langmead
Christopher J
CJ
Watson
Jeannette
J
Wu
Zining
Z
Forbes
Ian T
IT
Jin
Jian
J
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D055808:Drug Discovery; D006841:Hydrocarbons, Aromatic / Q000138:chemical synthesis* / Q000494:pharmacology; D015394:Molecular Structure; D043643:Receptor, Muscarinic M1 / Q000819:agonists*; D013329:Structure-Activity Relationship
D000577:Amides; D006841:Hydrocarbons, Aromatic; D043643:Receptor, Muscarinic M1