• Bioorg. Med. Chem. Lett. · Jun 2010

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

    • Brian Budzik, Vincenzo Garzya, Dongchuan Shi, Graham Walker, Yann Lauchart, Adam J Lucas, Ralph A Rivero, Christopher J Langmead, Jeannette Watson, Zining Wu, Ian T Forbes, and Jian Jin.
    • Discovery Research and Centers of Excellence for Drug Discovery, GlaxoSmithKline, Collegeville, PA 19426, USA. torqux@yahoo.com
    • Bioorg. Med. Chem. Lett. 2010 Jun 15; 20 (12): 3545-9.

    AbstractFurther 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.Copyright 2010 Elsevier Ltd. All rights reserved.

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