2′ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling

Article abstract of DOI:10.1016/j.bmcl.2010.04.127

Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M ₁ agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M₁ over M_2-5, and DMPK properties of these novel compounds are described.