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Antifungal promising agents of zinc(II) and copper(II) derivatives based on azole drug

de Azevedo-França, Jose Aleixo ; Borba-Santos, Luana Pereira ; de Almeida Pimentel, Giovana ; Franco, Chris Hebert Jesus ; Souza, Cassiano ; de Almeida Celestino, Jaqueline ; de Menezes, Emanuella Figueiredo ; dos Santos, Nathalia Pinheiro ; Vieira, Eduardo Guimarães ; Ferreira, Ana Maria Da Costa ; de Souza, Wanderley ; Rozental, Sonia ; Navarro, Maribel

Journal of inorganic biochemistry, 2021-06, Vol.219, p.111401-111401, Article 111401 [Periódico revisado por pares]

United States: Elsevier Inc

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Título:
Antifungal promising agents of zinc(II) and copper(II) derivatives based on azole drug
Autor: de Azevedo-França, Jose Aleixo ; Borba-Santos, Luana Pereira ; de Almeida Pimentel, Giovana ; Franco, Chris Hebert Jesus ; Souza, Cassiano ; de Almeida Celestino, Jaqueline ; de Menezes, Emanuella Figueiredo ; dos Santos, Nathalia Pinheiro ; Vieira, Eduardo Guimarães ; Ferreira, Ana Maria Da Costa ; de Souza, Wanderley ; Rozental, Sonia ; Navarro, Maribel
Assuntos: Antifungal Agents - chemistry ; Antifungal Agents - pharmacology ; Azoles - chemistry ; Candida albicans ; Candida albicans - drug effects ; Clotrimazole ; Clotrimazole - chemistry ; Clotrimazole - pharmacology ; Coordination Complexes - chemistry ; Coordination Complexes - pharmacology ; Copper - chemistry ; Cryptococcus neoformans ; Cryptococcus neoformans - drug effects ; Ketoconazole ; Ketoconazole - chemistry ; Ketoconazole - pharmacology ; Metal complexes ; Microbial Sensitivity Tests - methods ; Sporothrix - drug effects ; Sporothrix brasiliensis ; X-Ray Diffraction - methods ; Zinc - chemistry
É parte de: Journal of inorganic biochemistry, 2021-06, Vol.219, p.111401-111401, Article 111401
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SourceType-Scholarly Journals-1
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Descrição: A series of new metal complexes, [Zn(KTZ)2(Ac)2]·H2O (1), [Zn(KTZ)2Cl2]·0.4CH3OH (2), [Zn(KTZ)2(H2O)(NO3)](NO3) (3), [Cu(KTZ)2(Ac)2]·H2O (4), [Cu(KTZ)2Cl2]·3.2H2O (5), [Cu(KTZ)2(H2O)(NO3)](NO3)·H2O (6), were synthesized by a reaction of ketoconazole (KTZ) with their respective zinc or copper salts under mild conditions. Similarly, six corresponding metal-CTZ (clotrimazole) complexes [Zn(CTZ)2(Ac)2]·4H2O (7), [Zn(CTZ)2Cl2] (8), [Zn(CTZ)2(H2O)(NO3)](NO3)·4H2O (9), [Cu(CTZ)2(Ac)2]·H2O (10), [Cu(CTZ)2Cl2]·2H2O (11), [Cu(CTZ)2(H2O)(NO3)](NO3)·2H2O (12), were obtained. These metal complexes were characterized by elemental analyses, molar conductivity, 1H and 13C{1H} nuclear magnetic resonance, UV/Vis, and infrared spectroscopies. Further, the crystal structure for complexes 7 and 10 was determined by single-crystal X-ray diffraction. The antifungal activity of these metal complexes was evaluated against three fungal species of medical relevance: Candida albicans, Cryptococcus neoformans, and Sporothrix brasiliensis. Complexes 1 and 3 exhibited the greatest antifungal activity with a broad spectrum of action at low concentrations and high selectivity. Some morphological changes induced by these metal complexes in S. brasiliensis cells included yeast-hyphae conversion, an increase in cell size and cell wall damage. The strategy of coordination of clinic drugs (KTZ and CTZ) to zinc and copper was successful, since the corresponding metal complexes were more effective than the parent drug. Particularly, the promising antifungal activities displayed by Zn-KTZ complexes make them potential candidates for the development of an alternative drug to treat mycoses. A series of new Zn(II)/Cu(II)- azole drug complexes were synthesized, characterized and evaluated against three fungal species of medical relevance: Candida albicans, Cryptococcus neoformans, and Sporothrix brasiliensis. Zn(II)-KTZ (KTZ: Ketoconazole) complexes exhibited the greatest antifungal activity with a broad spectrum of action at low concentrations and high selectivity. [Display omitted] •Ten novel Zn(II)/Cu(II)-azole drug complexes were synthesized.•X-ray structure of two Zn(II)/Cu(II)-CTZ (CTZ: Clotrimazole) complexes were elucidated.•They were evaluated against three fungal species of medical relevance.•Zn(II)-KTZ (KTZ: Ketozonazole) complexes were the most effective antifungal agents.•They displayed high selectivity towards fungi over mammalian cells.
Editor: United States: Elsevier Inc
Idioma: Inglês

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Antifungal promising agents of zinc(II) and copper(II) derivatives based on azole drug

United States: Elsevier Inc

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