Albuquerque, HélioSantos, Clementina M.M.Silva, ArturCavaleiro, José2016-05-302016-05-302015Albuquerque, 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 978-989-98541-9-2978-989-98541-9-2http://hdl.handle.net/10198/12948The 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.engconference object