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The 1,2,4-triazolo[1,5-a][1,3,5]triazine system has been recognized as a promising scaffold for drug development purposes. The isosteric relationship between this skeleton and purines plays an important role in the research towards the development of bioactive 1,2,4-triazolo[1,5-a][1,3,5]triazine derivatives. This review discusses recently developed strategies for the synthesis of 1,2,4-triazolo[1,5-a][1,3,5]triazines and advances achieved in studies on biological activity of compounds constructed using this skeleton.
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