Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators.

Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2008 18 (20): 5626-30

PMID: 18793851 · PMCID: PMC3182458 · DOI:10.1016/j.bmcl.2008.08.087

This letter describes the synthesis and SAR, developed through an iterative analogue library approach, of an mGluR4 positive allosteric modulator lead based on a pyrazolo[3,4-d]pyrimidine scaffold. Despite tremendous therapeutic potential, Compound 7, VU0080421, and related congeners represent only a handful of mGluR4 positive allosteric modulators ever described.

MeSH Terms (15)

Allosteric Regulation Allosteric Site Animals Chemistry, Pharmaceutical CHO Cells Cricetinae Cricetulus Dose-Response Relationship, Drug Drug Design Glutamic Acid Models, Chemical Neurotransmitter Agents Pyrimidines Receptors, Metabotropic Glutamate Structure-Activity Relationship

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