Preparation of a series of 5-methyl-3-(substituted)-[1,2,4]triazines

TETRAHEDRON LETTERS

卷:52

Article

Gichinga, Moses G.¹  Olson, Jeremy P.¹  Butala, Elizabeth¹  Gilmour, Brian P.¹  Navarro, Hernan H.¹  Carroll, F. Ivy¹ 

[1] Res Triangle Inst, Ctr Organ & Med Chem, Res Triangle Pk, NC 27709 USA

关键词: Triazine;    mGluR5 antagonist;    Addiction;    Heterocyclic synthesis;   

DOI  :  10.1016/j.tetlet.2011.04.075

来源: Elsevier

【 摘 要 】

Procedures for the synthesis of thirty-six 5-methyl-3-(substituted)-[1,2,4]triazines have been described. These compounds were evaluated for antagonism at metabotropic glutamate receptor subtype 5 (mGluR5). Two compounds, 5b and 3c, were determined to be low micromolar inhibitors of mGluR5. (C) 2011 Elsevier Ltd. All rights reserved.

【 授权许可】

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