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Bioorg Med Chem Lett. 2008 Feb 1;18(3):885-90. doi: 10.1016/j.bmcl.2007.12.051. Epub 2008 Jan 4.

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

Author information

1
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.

PMID:
18178088
PMCID:
PMC2275053
DOI:
10.1016/j.bmcl.2007.12.051
[Indexed for MEDLINE]
Free PMC Article

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