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

Author(s)

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

• Document type: Journal article
• Source: Journal of Inorganic Biochemistry; v. 233, p. 12-pg., 2022-04-29.

Abstract

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)

• FAPESP's process: 16/16735-8 - Imobilization of potential metallopharmaceuticals in inorganic and organic matrices for modified delivery
• Grantee: Eduardo Guimarães Vieira
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 13/07937-8 - Redoxome - Redox Processes in Biomedicine
• Grantee: Ohara Augusto
• Support Opportunities: Research Grants - Research, Innovation and Dissemination Centers - RIDC