Bioorganic & medicinal chemistry letters
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Bioorg. Med. Chem. Lett. · Jun 2010
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.
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 M(1) over M(2-5), and DMPK properties of these novel compounds are described.