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

Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2008 18 (3): 885-90

PMID: 18178088 · PMCID: PMC2275053 · DOI:10.1016/j.bmcl.2007.12.051

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.

MeSH Terms (12)

Combinatorial Chemistry Techniques Dose-Response Relationship, Drug Dystonia Heterocyclic Compounds Humans Molecular Structure Muscarinic Antagonists Parkinson Disease Receptor, Muscarinic M1 Receptors, G-Protein-Coupled Receptors, Muscarinic Structure-Activity Relationship

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