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Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.

Melancon BJ, Utley TJ, Sevel C, Mattmann ME, Cheung YY, Bridges TM, Morrison RD, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR
Bioorg Med Chem Lett. 2012 22 (15): 5035-40

PMID: 22749871 · PMCID: PMC3883446 · DOI:10.1016/j.bmcl.2012.06.018

This Paper describes the continued optimization of an MLPCN probe molecule M(1) antagonist (ML012) through an iterative parallel synthesis approach. After several rounds of modifications of the parent compound, we arrived at a new azetidine scaffold that displayed improved potency while maintaining a desirable level of selectivity over other muscarinic receptor subtypes. Data for representative molecules 7w (VU0452865) and 12a (VU0455691) are presented.

Copyright © 2012 Elsevier Ltd. All rights reserved.

MeSH Terms (13)

Animals Azabicyclo Compounds Azetidines Cytochrome P-450 Enzyme System Humans Molecular Probes Protein Binding Protein Isoforms Rats Receptor, Muscarinic M1 Structure-Activity Relationship Sulfonamides Thiadiazoles

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