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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1044-8. doi: 10.1016/j.bmcl.2011.11.110. Epub 2011 Dec 6.

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

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

Abstract

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.

PMID:
22197142
[PubMed - indexed for MEDLINE]
PMCID:
PMC3434972
Free PMC Article
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