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Issue 11, 2011
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Synthesis and evaluation of 1,2,4-methyltriazines as mGluR5 antagonists

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Abstract

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.

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

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Article information


Submitted
16 Dec 2010
Accepted
23 Mar 2011
First published
24 Mar 2011

Org. Biomol. Chem., 2011,9, 4276-4286
Article type
Paper

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

J. P. Olson, M. G. Gichinga, E. Butala, H. A. Navarro, B. P. Gilmour and F. I. Carroll, Org. Biomol. Chem., 2011, 9, 4276
DOI: 10.1039/C0OB01190H

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