Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.

Bridges TM, Kennedy JP, Hopkins CR, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2010 20 (19): 5617-22

PMID: 20801651 · PMCID: PMC3179183 · DOI:10.1016/j.bmcl.2010.08.042

This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M(5)-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan G(q) mAChR M(1), M(3), M(5) PAM. An iterative parallel synthesis approach was employed to incorporate basic heterocycles to improve physiochemical properties.

Copyright (c) 2010 Elsevier Ltd. All rights reserved.

MeSH Terms (11)

Allosteric Regulation Animals CHO Cells Cricetinae Cricetulus Ethers Heterocyclic Compounds High-Throughput Screening Assays Humans Receptors, Muscarinic Structure-Activity Relationship

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