Synthesis and evaluation of 1,2,4-methyltriazines as mGluR5 antagonists

Jeremy P. Olson; Moses G. Gichinga; Elizabeth Butala; Hernan A. Navarro; Brian P. Gilmour; F. Ivy Carroll

doi:10.1039/C0OB01190H

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Organic & Biomolecular Chemistry

Issue 11, 2011

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Synthesis and evaluation of 1,2,4-methyltriazines as mGluR5 antagonists

Jeremy P. Olson , Moses G. Gichinga , Elizabeth Butala , Hernan A. Navarro , Brian P. Gilmour and F. Ivy Carroll

Org. Biomol. Chem., 2011,9, 4276-4286

DOI: 10.1039/C0OB01190H
Received 16 Dec 2010, Accepted 23 Mar 2011
First published on the web 24 Mar 2011

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In previous studies we showed that 3-(substituted phenylethynyl)-5-methyl[1,2,4]triazine analogues of MPEP were potent antagonists of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro efficacy assay. In the present study we report the synthesis and evaluation of six 3-(substituted biphenylethynyl)-5-methyl[1,2,4]triazines (5a–f), and five 3-(substituted phenoxyphenylethynyl)-5-methyltriazines (6a–e). Compound 2-(4-fluorophenyl-5-[2-(5-methyl[1,2,4]triazine-3-yl)ethynyl]benzonitrile (5f) with an IC₅₀ of 28.2 nM was the most potent analogue.