Synthesis and Biological Activity of Novel Zinc-Itraconazole Complexes in Protozoan Parasites and Sporothrix spp

The new complexes Zn(ITZ) Cl (1) and Zn(ITZ) (OH) (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, H and C{ H} nuclear magnetic resonance, and UV-v...

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Published in:Antimicrobial agents and chemotherapy 2020-04, Vol.64 (5)
Main Authors: Azevedo-França, Jose Aleixo de, Granado, Renato, de Macedo Silva, Sara Teixeira, Santos-Silva, Gabrielle Dos, Scapin, Sandra, Borba-Santos, Luana P, Rozental, Sonia, de Souza, Wanderley, Martins-Duarte, Érica S, Barrias, Emile, Rodrigues, Juliany Cola Fernandes, Navarro, Maribel
Format: Article
Language:English
Subjects:
Antifungal Agents - pharmacology
Antiparasitic Agents - pharmacology
Itraconazole - pharmacology
Leishmania - drug effects
Leishmania mexicana - drug effects
Microbial Sensitivity Tests
Parasitic Sensitivity Tests
Sporothrix - drug effects
Susceptibility
Toxoplasma - drug effects
Trypanosoma cruzi - drug effects
Zinc - pharmacology
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Summary:The new complexes Zn(ITZ) Cl (1) and Zn(ITZ) (OH) (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, H and C{ 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, , , and , and two fungi, namely, and 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.
ISSN:0066-4804
1098-6596
DOI:10.1128/AAC.01980-19