Open AccessSynthesis and Biological Activity of Novel Zinc-Itraconazole Complexes in Protozoan Parasites and Sporothrix spp
Author(s) -
José Aleixo de Azevedo-França,
Renato Granado,
Sara Teixeira de Macedo Silva,
Gabrielle Dos Santos-Silva,
Sandra Mara Naressi Scapin,
Luana Pereira Borba-Santos,
Sônia Rozental,
Wanderley de Souza,
Érica S. Martins-Duarte,
Emile Barrias,
Juliany Cola Fernandes Rodrigues,
Maribel Navarro
Publication year - 2020
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.01980-19
Subject(s) - itraconazole , zinc , sporothrix , antiparasitic , microbiology and biotechnology , leishmania braziliensis , nuclear chemistry , chemistry , sporothrix schenckii , leishmania , leishmaniasis , biology , antifungal , parasite hosting , sporotrichosis , organic chemistry , cutaneous leishmaniasis , immunology , pathology , medicine , world wide web , computer science
The new complexes Zn(ITZ) 2 Cl 2 (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 and 13 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.