Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs.

@article{Wenthur2014SynthesisAS,
  title={Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs.},
  author={Cody J Wenthur and Ryan D. Morrison and John Scott Daniels and P Jeffrey Conn and Craig W Lindsley},
  journal={Bioorganic & medicinal chemistry letters},
  year={2014},
  volume={24 12},
  pages={2693-8}
}
Herein we report the design and synthesis of a series of substituted pyrazolo[1,5-a]quinazolin-5(4H)-ones as negative allosteric modulators of metabotropic glutamate receptors 2 and 3 (mGlu2 and mGlu3, respectively). Development of this series was initiated by reports that pyrazolo[1,5-a]quinazoline-derived scaffolds can yield compounds with activity at group II mGlu receptors which are prone to molecular switching following small structural changes. Several potent analogues, including 4-methyl… CONTINUE READING