2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. doi: 10.1016/j.bmcl.2008.08.087.
Colleen M Niswender 1,  Evan P Lebois,  Qingwei Luo,  Kwangho Kim,  Hubert Muchalski,  Huiyong Yin,  P Jeffrey Conn,  Craig W Lindsley
Affiliations

Affiliation

  • 1 Department of Pharmacology, Vanderbilt University Medical Center, 802 Robinson Research Building, Nashville, TN 37232-6600, USA.
PMID: 18793851 DOI: 10.1016/j.bmcl.2008.08.087
Abstract

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.

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