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

被引：26

作者：

de Azevedo-Franca, Jose Aleixo ^{[1
]}

Granado, Renato ^{[2
]}

de Macedo Silva, Sara Teixeira ^{[3
]}

dos Santos-Silva, Gabrielle ^{[3
,4
]}

Scapin, Sandra ^{[2
]}

Borba-Santos, Luana P. ^{[5
]}

Rozental, Sonia ^{[5
]}

de Souza, Wanderley ^{[3
]}

Martins-Duarte, Erica S. ^{[6
]}

Barrias, Emile ^{[2
]}

Fernandes Rodrigues, Juliany Cola ^{[3
,4
]}

Navarroa, Maribel ^{[1
,2
]}

机构：

[1] Univ Fed Juiz de Fora, Dept Quim, ICE, Juiz De Fora, Brazil

[2] INMETRO, Diretoria Metrol Aplicada Ciencias Vida, Inst Nacl Metrol Qualidade & Tecnol, Xerem, Brazil

[3] Univ Fed Rio de Janeiro, Lab Ultraestrutura Celular Hertha Meyer, Inst Biofis Carlos Chagas Filho, Rio De Janeiro, Brazil

[4] Univ Fed Rio de Janeiro, Nucleo Multidisciplinar Pesquisa Biol, NUMPEX Bio, Campus UFRJ Duque Caxias Prof Geraldo Cidade, Rio De Janeiro, Brazil

[5] Univ Fed Rio de Janeiro, Lab Biol Celular Fungos, Inst Biofis Carlos Chagas Filho, Rio De Janeiro, Brazil

[6] Univ Fed Minas Gerais, Dept Parasitol, Inst Ciencias Biol, Belo Horizonte, MG, Brazil

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2020年 / 64卷 / 05期

关键词：

itraconazole; zinc; Trypanosoma cruzi; Leishmania amazonensis; Toxoplasma gondii; Sporothrix spp; AGENTS; TRYPANOSOMIASIS; LEISHMANIASIS; MALARIA;

D O I：

10.1128/AAC.01980-19

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

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, H-1 and C-13{H-1} 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.

引用

页数：15

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