Synthesis and biological characterization of a series of novel diaryl amide M 1 antagonists

…, JS Daniels, PJ Conn, CW Lindsley, MR Wood

Index: Poslusney, Michael S.; Sevel, Christian; Utley, Thomas J.; Bridges, Thomas M.; Morrison, Ryan D.; Kett, Nathan R.; Sheffler, Douglas J.; Niswender, Colleen M.; Daniels, J. S.; Conn, P. J.; Lindsley, Craig W.; Wood, Michael R. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 22 p. 6923 - 6928,6

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Citation Number: 2

Abstract

Utilizing a combination of high-throughput and multi-step synthesis, SAR in a novel series of M1 acetylcholine receptor antagonists was rapidly established. The efforts led to the discovery the highly potent M1 antagonists 6 (VU0431263), and 8f (VU0433670). Functional Schild analysis and radioligand displacement experiments demonstrated the competitive, orthosteric binding of these compounds; human selectivity data are presented.