Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594506 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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.
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Authors
Michael S. Poslusney, Christian Sevel, Thomas J. Utley, Thomas M. Bridges, Ryan D. Morrison, Nathan R. Kett, Douglas J. Sheffler, Colleen M. Niswender, J.S. Daniels, P.J. Conn, Craig W. Lindsley, Michael R. Wood,