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Bioorg Med Chem Lett. 2011 Jun 1;21(11):3243-7. doi: 10.1016/j.bmcl.2011.04.047. Epub 2011 Apr 20.

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

Author information

1
Institute for Neurodegenerative Disorders, 60 Temple St., Suite 8A, New Haven, CT 06510, USA. dalagille@indd.org

Erratum in

  • Bioorg Med Chem Lett. 2012 Mar 1;22(5):2130. Conn, Jeffrey P [corrected to Conn, P Jeffrey].

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.

PMID:
21546249
PMCID:
PMC3826776
DOI:
10.1016/j.bmcl.2011.04.047
[Indexed for MEDLINE]
Free PMC Article

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