Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5

Andrew S. Felts, Sam A. Saleh, Uyen Le, Alice L. Rodriguez, C. David Weaver, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte

Research output: Contribution to journalArticle

15 Scopus citations

Abstract

A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of metabotropic glutamate receptor 5 (mGlu5). This Letter describes the SAR of this series and the profile of selected compounds in selectivity and radioligand binding assays.

Original languageEnglish
Pages (from-to)6623-6626
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number23
DOIs
StatePublished - 1 Dec 2009

Keywords

  • Glutamate
  • Metabotropic glutamate receptor 5
  • Negative allosteric modulator
  • Non-competitive antagonist
  • Quinazoline

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