2. Academic Validation
  3. Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series

Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series

  • Bioorg Med Chem Lett. 2011 Jun 1;21(11):3243-7. doi: 10.1016/j.bmcl.2011.04.047.
David Alagille 1,  Herve DaCosta,  Yelin Chen,  Kamondanai Hemstapat,  Alice Rodriguez,  Ronald M Baldwin,  P Jeffrey Conn,  Gilles D Tamagnan
Affiliations

Affiliation

  • 1 Institute for Neurodegenerative Disorders, 60 Temple St., Suite 8A, New Haven, CT 06510, USA. dalagille@indd.org
PMID: 21546249 DOI: 10.1016/j.bmcl.2011.04.047
Abstract

We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl)ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.

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