Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.

  title={Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.},
  author={Michael S. Poslusney and Christian Sevel and Thomas J. Utley and Thomas M. Bridges and Ryan D. Morrison and Nathan R. Kett and Douglas J. Sheffler and Colleen M. Niswender and John Scott Daniels and P. Jeffrey Conn and Craig W. Lindsley and Michael R. Wood},
  journal={Bioorganic \& medicinal chemistry letters},
  volume={22 22},
Utilizing a combination of high-throughput and multi-step synthesis, SAR in a novel series of M(1) acetylcholine receptor antagonists was rapidly established. The efforts led to the discovery the highly potent M(1) 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. 
5 Citations
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