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

21 Citations (Scopus)

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

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Ether
Modulators
1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione

Keywords

  • Allosteric
  • M5
  • PAM
  • mAChR

ASJC Scopus subject areas

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

Cite this

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. / Bridges, Thomas M.; Kennedy, J. Phillip; Hopkins, Corey R; Conn, P. Jeffrey; Lindsley, Craig W.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 19, 01.10.2010, p. 5617-5622.

Research output: Contribution to journalArticle

Bridges, Thomas M. ; Kennedy, J. Phillip ; Hopkins, Corey R ; Conn, P. Jeffrey ; Lindsley, Craig W. / Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 19. pp. 5617-5622.
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