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Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists |
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| Authors: | 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 |
| Affiliation: | Vanderbilt Program in Drug Discovery, Vanderbilt Institute of Chemical Biology, Nashville, TN 37232, USA. |
| Abstract: | This Letter describes the synthesis and SAR, developed through an iterative analogue library approach, of a novel series of selective M1 mAChR antagonists 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 441nM-19microM range with 8- to >340-fold functional selectivity versus rM2-rM5. |
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