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Bioorg Med Chem Lett. 2010 Apr 1;20(7):2174-7. doi: 10.1016/j.bmcl.2010.02.041. Epub 2010 Feb 13.

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

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1
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.

Abstract

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).

PMID:
20202841
PMCID:
PMC2843780
DOI:
10.1016/j.bmcl.2010.02.041
[Indexed for MEDLINE]
Free PMC Article

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