Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369783 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
This Letter describes the continued optimization of the MLPCN probe molecule ML071. After introducing numerous cyclic constraints and novel substitutions throughout the parent structure, we produced a number of more highly potent agonists of the M1 mACh receptor. While many novel agonists demonstrated a promising ability to increase soluble APPα release, further characterization indicated they may be functioning as bitopic agonists. These results and the implications of a bitopic mode of action are presented.
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Related Topics
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Organic Chemistry
Authors
Bruce J. Melancon, Rocco D. Gogliotti, James C. Tarr, Sam A. Saleh, Brian A. Chauder, Evan P. Lebois, Hyekyung P. Cho, Thomas J. Utley, Douglas J. Sheffler, Thomas M. Bridges, Ryan D. Morrison, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn,