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

J Inorg Biochem

Laboratório de Química Bioinorgânica e Catálise, Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Juiz de Fora, MG. Brazil. Electronic address:

Published: August 2022

AI Article Synopsis

  • A series of transition metal coordination polymers containing zinc and copper were synthesized using fluconazole and various metal salts under mild conditions, resulting in six new compounds.
  • The structures of these compounds were confirmed through various analytical techniques, including single-crystal X-ray diffraction for four of the compounds.
  • The compounds showed significant antichagasic activity against Trypanosoma cruzi, with one compound (2) being particularly effective, suggesting that these coordination polymers could be better therapeutic options than the free azole drug for Chagas disease.

Article Abstract

A series of new transition metal coordination polymers, [Zn(Ac)(FLZ)] (1) [Zn(FLZ)(Cl)] (2), {[Zn(FLZ)](NO)} (3), [Cu(FLZ)(CH₃COO)] (4) {[Cu(FLZ)Cl]} (5) and {[Cu(FLZ)](NO)} (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 and C{H} 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.

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Source
http://dx.doi.org/10.1016/j.jinorgbio.2022.111834DOI Listing

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