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
  • 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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