Promising fluconazole based zinc(II) and copper(II) coordination polymers against Chagas disease

Autor(es)

De Azevedo-Franca, Jose Aleixo ; Barrias, Emile ; Franco, Chris Hebert Jesus ; Villarreal, Wilmer ; Vieira, Eduardo Guimaraes ; Da Costa Ferreira, Ana Maria ; de Souza, Wanderley ; Navarro, Maribel

• Tipo de documento: Artigo Científico
• Fonte: Journal of Inorganic Biochemistry; v. 233, p. 12-pg., 2022-04-29.

Resumo

A series of new transition metal coordination polymers, [Zn(Ac)(2)(FLZ)(2)](n) (1), [Zn(FLZ)(2)(Cl)(2)](n) (2), {[Zn(FLZ)(2)] (NO3)(2)}(n) (3), [Cu(FLZ)(2)(CH3COO)(4)](n) (4), {[Cu(FLZ)(2)Cl-2]}(n) (5) and {[Cu(FLZ)(2)](NO3)(2)}(n) (6), were synthesized by the reaction of fluconazole (FLZ) with the respective zinc or copper salts under mild conditions. The molecular structure of these compounds was elucidated by several analytical and spectroscopy techniques such as elemental analyses, H-1 and C-13{H-1} nuclear magnetic resonance, electronic paramagnetic resonance, and infrared spectroscopy. Single-crystal X-ray diffraction confirmed the structure of the compounds 2, 4, 5 and 6 in solid state. The antichagasic activity of these compounds was evaluated against different forms of Trypanosoma cruzi. Compound 2 exhibited the highest activity against intracellular amastigotes. The ultrastructural changes in epimastigotes and intracellular amastigotes were investigated. These promising biological results demonstrated that the zinc or copper coordination polymers can form very active anti-parasitic compounds. The resulting compounds are more effective than the free azole drug and, consequently, great candidates for the treatment of Chagas disease. (AU)

• Processo FAPESP: 16/16735-8 - Imobilização de potenciais metalofármacos em matrizes inorgânicas ou orgânicas para liberação modificada
• Beneficiário: Eduardo Guimarães Vieira
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 13/07937-8 - Redoxoma
• Beneficiário: Ohara Augusto
• Modalidade de apoio: Auxílio à Pesquisa - Centros de Pesquisa, Inovação e Difusão - CEPIDs