Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkins

@article{Jones2011DiscoverySA,
  title={Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkins},
  author={Carrie K Jones and Darren W Engers and Analisa D. Thompson and Julie R. Field and Anna L Blobaum and Stacey Lindsley and Ya Li Zhou and Rocco D. Gogliotti and Satyawan Jadhav and R. Ariel Zamorano and Jim Bogenpohl and Yoland Smith and Ryan D. Morrison and John Scott Daniels and C David Weaver and P Jeffrey Conn and Craig W Lindsley and Colleen M Niswender and Corey R Hopkins},
  journal={Journal of medicinal chemistry},
  year={2011},
  volume={54 21},
  pages={7639-47}
}
There is an increasing amount of literature data showing the positive effects on preclinical antiparkinsonian rodent models with selective positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)). However, most of the data generated utilize compounds that have not been optimized for druglike properties, and as a consequence, they exhibit poor pharmacokinetic properties and thus do not cross the blood-brain barrier. Herein, we report on a series of N-4-(2,5-dioxopyrrolidin-1… CONTINUE READING

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