Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) anatgonists

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) anatgonists

This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of a novel series of selective M1 mAChR antagonist for the potential treatment of Parkinson’s disease, dystonia and other movement disorders. Compounds in this series possess M1 antagonist IC 50 s in...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2008-01, Vol.18 (3), p.885-890
Hauptverfasser: Lewis, L. Michelle, Sheffler, Douglas, Williams, Richard, Bridges, Thomas M., Kennedy, J. Phillip, Brogan, J.T., Mulder, Matthew J., Williams, Lyndsey, Nalywajko, Natalia T., Niswender, Colleen M., Weaver, Charles D., Conn, P. Jeffrey, Lindsley, Craig W.
Format: Artikel
Sprache:eng
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Zusammenfassung:This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of a novel series of selective M1 mAChR antagonist for the potential treatment of Parkinson’s disease, dystonia and other movement disorders. Compounds in this series possess M1 antagonist IC 50 s in the 441 nM to 19 µM range with 8- to >340-fold functional selectivity versus rM2–rM5.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.12.051