Synthèse et étude physicochimique des complexes d’une molécule médicamenteuse avec des agents complexants

Abstract

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.