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

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. doi: 10.1016/j.bmcl.2009.10.024. Epub 2009 Oct 9.

Abstract

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

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Drug Design
  • Drug Discovery*
  • Humans
  • Molecular Structure
  • Quinazolines / chemical synthesis
  • Quinazolines / chemistry
  • Quinazolines / pharmacology*
  • Rats
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Quinazolines
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate