4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 12, Pages 3540-3544

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.128

Keywords

Subtype selective M1 muscarinic; acetylcholine receptor agonist; Novel M1 agonists; 2 ' Biaryl amides

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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 M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2-5, are described. (C) 2010 Elsevier Ltd. All rights reserved.

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