Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

Thomas M. Bridges, J. Phillip Kennedy, Corey R. Hopkins, P. Jeffrey Conn, Craig W. Lindsley

Research output: Contribution to journalArticle

22 Scopus citations

Abstract

This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M5-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan Gq mAChR M1, M3, M5 PAM. An iterative parallel synthesis approach was employed to incorporate basic heterocycles to improve physiochemical properties.

Original languageEnglish (US)
Pages (from-to)5617-5622
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number19
DOIs
StatePublished - Oct 1 2010

Keywords

  • Allosteric
  • M5
  • PAM
  • mAChR

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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