1. Synthesis and Biological Activity of Novel Zinc-Itraconazole Complexes in Protozoan Parasites and Sporothrix spp.
- Author
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Azevedo-França JA, Granado R, de Macedo Silva ST, Santos-Silva GD, Scapin S, Borba-Santos LP, Rozental S, de Souza W, Martins-Duarte ÉS, Barrias E, Rodrigues JCF, and Navarro M
- Subjects
- Leishmania drug effects, Leishmania mexicana drug effects, Microbial Sensitivity Tests, Parasitic Sensitivity Tests, Sporothrix drug effects, Toxoplasma drug effects, Trypanosoma cruzi drug effects, Antifungal Agents pharmacology, Antiparasitic Agents pharmacology, Itraconazole pharmacology, Zinc pharmacology
- Abstract
The new complexes Zn(ITZ)
2 Cl2 (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,1 H and13 C{1 H} 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, Leishmania amazonensis , Trypanosoma cruzi , and Toxoplasma gondii , and two fungi, namely, Sporothrix brasiliensis and Sporothrix schenckii 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., (Copyright © 2020 American Society for Microbiology.)- Published
- 2020
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