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Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.

Melancon BJ, Lamers AP, Bridges TM, Sulikowski GA, Utley TJ, Sheffler DJ, Noetzel MJ, Morrison RD, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Wood MR
Bioorg Med Chem Lett. 2012 22 (2): 1044-8

PMID: 22197142 · PMCID: PMC3434972 · DOI:10.1016/j.bmcl.2011.11.110

This Letter describes the continued optimization of an MLPCN probe molecule (ML012) through an iterative parallel synthesis approach. After exploring extensive modifications throughout the parent structure, we arrived at a more highly M(1)-selective antagonist, compound 13l (VU0415248). Muscarinic subtype selectivity across all five human and rat receptors for 13l, along with rat selectivity for the lead compound (ML012), is presented.

Copyright © 2011 Elsevier Ltd. All rights reserved.

MeSH Terms (10)

Animals Dose-Response Relationship, Drug Humans Molecular Probes Molecular Structure Quinolines Rats Receptor, Muscarinic M1 Structure-Activity Relationship Sulfonamides

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