Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu4) with CNS exposure in rats

Darren W. Engers, Julie R. Field, Uyen Le, Ya Zhou, Julie D. Bolinger, Rocio Zamorano, Anna L. Blobaum, Carrie K. Jones, Satyawan Jadhav, C. David Weaver, P. Jeffrey Conn, Craig W. Lindsley, Colleen M. Niswender, Corey R. Hopkins

Research output: Contribution to journalArticle

33 Scopus citations

Abstract

Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpicolinamides as positive allosteric modulators of mGlu4. Compounds from the series show submicromolar potency at both human and rat mGlu4. In addition, pharmacokinetic studies utilizing subcutaneous dosing demonstrated good brain exposure in rats.

Original languageEnglish (US)
Pages (from-to)1106-1110
Number of pages5
JournalJournal of Medicinal Chemistry
Volume54
Issue number4
DOIs
Publication statusPublished - Feb 24 2011

    Fingerprint

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this