Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.

Poslusney MS, Sevel C, Utley TJ, Bridges TM, Morrison RD, Kett NR, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR
Bioorg Med Chem Lett. 2012 22 (22): 6923-8

PMID: 23062550 · PMCID: PMC3897205 · DOI:10.1016/j.bmcl.2012.09.011

Utilizing a combination of high-throughput and multi-step synthesis, SAR in a novel series of M(1) acetylcholine receptor antagonists was rapidly established. The efforts led to the discovery the highly potent M(1) antagonists 6 (VU0431263), and 8f (VU0433670). Functional Schild analysis and radioligand displacement experiments demonstrated the competitive, orthosteric binding of these compounds; human selectivity data are presented.

Copyright © 2012 Elsevier Ltd. All rights reserved.

MeSH Terms (13)

Acetylcholine Amides Animals Binding, Competitive CHO Cells Cricetinae Cricetulus Humans Piperazines Receptor, Muscarinic M1 Stereoisomerism Stilbenes Structure-Activity Relationship

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