2. Academic Validation
  3. Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

  • Bioorg Med Chem Lett. 2010 Oct 1;20(19):5617-22. doi: 10.1016/j.bmcl.2010.08.042.
Thomas M Bridges 1,  J Phillip Kennedy,  Corey R Hopkins,  P Jeffrey Conn,  Craig W Lindsley
Affiliations

Affiliation

  • 1 Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
PMID: 20801651 DOI: 10.1016/j.bmcl.2010.08.042
Abstract

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.

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