Résumé:
BASDENE is a commercialized drug active against hyperthyroidism. It is a thioamide, closely related to
propylthiouracil, it blocks thyroid hormone genesis by inhibiting the organification of iodine and it causes
hypersecretion of TSH. However, its low water solubility leads to a decrease in its biological activity. Recent
research has shown that complexing biologically active molecules with transition metals dramatically increases
their biological activity. On the other hand, complexion with cyclodextrins (CDs) is one of the most widely used
approaches to improve the water solubility of several drugs. In this work, we synthesized and characterized three
types of basdene complexes:
1) Inclusion complexes of 1: 1 and 2: 1 stoichiometry (Host: Guest) with β-cyclodextrin (β-CD).
2) 1: 1 and 1: 2 stoichiometric coordination complexes (Metal: Ligand) with zinc (Zn).
3) Inclusion complexes of 1: 1: 1 and 2: 1: 2 stoichiometric coordination complexes (Ligand: Metal: CD). This
type of complex was synthesized for the first time in order to have both more effective products, having better
biological activity due to the presence of a transition metal and more water-soluble following complexion with a
CD. The synthesized complexes were characterized in the solid state by IR spectroscopy, UV-visible
spectrophotometry, melting point, TLC and color. Each of these characterizations brought several elements
supporting the thesis of the formation of the different complexes studied.
