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

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.

Automated summary

A series of new transition metal coordination polymers were synthesized and their structures were elucidated. These coordination polymers exhibited promising anti-parasitic activity, surpassing the free azole drug. Therefore, they are potential candidates for the treatment of Chagas disease.