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Advisor(s)
Abstract(s)
The development of multi-target drugs for treating complex multifactorial diseases constitutes an active
research ield. This kind of drugs has gained much importance as alternative strategy to combination therapy
(“cocktail drugs”).1 A common way to design them brings together two different pharmacophores in one
single molecule (so-called dyads). Following this idea and being aware that xanthones2 and 1,2,3-triazoles3
possess important pharmacological properties, we combined these two heterocycles in one molecule to
create new dyads with improved therapeutic potential. In this work, new xanthone-1,2,3-triazole dyads were
prepared from novel (E)-2-(4-arylbut-1-en-3-yn-1-yl)chromones by two different approaches to evaluate
their eficiency and sustainability. Both methodologies involved Diels-Alder reactions to build the xanthone
core, which were optimized using microwave irradiation as alternative heating method, and 1,3-dipolar cycloadditions to insert the 1,2,3-triazole moiety (Figure 1).4 All final and intermediate compounds were fully
characterized by 1D and 2D NMR techniques.
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Pedagogical Context
Citation
Albuquerque, Hélio; Santos, Clementina M.M.; Silva, Artur M. S.; Cavaleiro, J. A. S. (2015). Recent developments in the synthesis of novel xanthone-1,2,3-triazole dyads. In 11º Encontro Nacional de Química Orgânica e 4º Encontro de Química Terapêutica. Porto. ISBN 978-989-98541-9-2