Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Juiz de Fora, Brazil.
Diretoria de Metrologia Aplicada a Ciências da Vida, Instituto Nacional de Metrologia, Qualidade e Tecnologia, INMETRO, Xerem, Brazil.
Antimicrob Agents Chemother. 2020 Apr 21;64(5). doi: 10.1128/AAC.01980-19.
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.
新的配合物 Zn(ITZ)Cl（1）和 Zn(ITZ)(OH)（2）是通过在回流条件下将伊曲康唑与相应的锌盐反应合成的。这些 Zn-ITZ 配合物通过元素分析、摩尔电导率、质谱、H 和 C{H} 核磁共振以及紫外可见和红外光谱进行了表征。评估了 Zn-ITZ 配合物对三种具有医学重要性的原生动物、即、、和两种真菌、即、和的抗寄生虫和抗真菌活性。Zn-ITZ 配合物表现出广谱作用，在低浓度下具有抗寄生虫和抗真菌活性。将锌与 ITZ 结合的策略有效地增强了 ITZ 的活性，因为 Zn-ITZ 配合物比单独的唑类更具活性。这项研究为未来将这些 Zn-ITZ 配合物应用于寄生虫病和孢子丝菌病的治疗开辟了前景。
