Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists |
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| Authors: | Nicole R. Miller R. Nathan Daniels David Lee P. Jeffrey Conn Craig W. Lindsley |
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| Affiliation: | 1. Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA;2. Vanderbilt Program in Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA;3. Vanderbilt MLPCN Specilaized Chemistry Center, Vanderbilt University Medical Center, Nashville, TN 37232, USA;4. Vanderbilt Institute of Chemical Biology, Vanderbilt University Medical Center, Nashville, TN 37232, USA;5. Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA |
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| Abstract: | This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of a novel series of selective M1 mAChR antagonists, based on an N-(4-(4-alkylpiperazin-1-yl)phenyl)benzamide scaffold for the potential treatment of Parkinson’s disease, dystonia and other movement disorders. Compounds in this series possess M1 antagonist IC50s in the 350 nM to >10 μM range with varying degrees of functional selectivity versus M2–M5. |
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