Synthesis and Biological Activity of Novel Zinc-Itraconazole Complexes in Protozoan Parasites and <i>Sporothrix</i> spp

Abstract

The new complexes Zn(ITZ)₂Cl₂ (1) and Zn(ITZ)₂(OH)₂ (2) were synthetized by a reaction of itraconazole with their respective zinc salts under reflux. These Zn-ITZ complexes were characterized by elemental analyses, molar conductivity, mass spectrometry, ¹H and ¹³C{¹H} nuclear magnetic resonance, and UV-vis and infrared spectroscopies. The antiparasitic and antifungal activity of Zn-ITZ complexes was evaluated against three protozoans of medical importance, namely, <i>Leishmania amazonensis</i>, <i>Trypanosoma cruzi</i>, and <i>Toxoplasma gondii</i>, and two fungi, namely, <i>Sporothrix brasiliensis</i> and <i>Sporothrix schenckii</i> The Zn-ITZ complexes exhibited a broad spectrum of action, with antiparasitic and antifungal activity in low concentrations. The strategy of combining zinc with ITZ was efficient to enhance ITZ activity since Zn-ITZ-complexes were more active than the azole alone. This study opens perspectives for future applications of these Zn-ITZ complexes in the treatment of parasitic diseases and sporotrichosis.