Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.

Miller NR, Daniels RN, Lee D, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2010 20 (7): 2174-7

PMID: 20202841 · PMCID: PMC2843780 · DOI:10.1016/j.bmcl.2010.02.041

This Letter describes the synthesis and SAR, developed through an iterative analog library approach, of a novel series of selective M(1) 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 M(1) antagonist IC(50)s in the 350 nM to >10 microM range with varying degrees of functional selectivity versus M(2)-M(5).

2010 Elsevier Ltd. All rights reserved.

MeSH Terms (13)

Amino Acid Sequence Animals Benzamides CHO Cells Cricetinae Cricetulus Dystonia Humans Mice Molecular Sequence Data Parkinson Disease Receptor, Muscarinic M1 Structure-Activity Relationship

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