New Copper (II) Complexes Based on 1,4-Disubstituted-1,2,3-Triazole Ligands with Promising Antileishmanial Activity.

Area of Science:

• Medicinal Chemistry
• Parasitology
• Computational Chemistry

Background:

• Leishmaniasis is a fatal parasitic disease with limited, side-effect-prone treatments.
• Current antileishmanial drugs exhibit inconsistent efficacy and significant adverse effects.

Purpose of the Study:

• To design and synthesize novel copper(II) triazole complexes as potential antileishmanial agents.
• To evaluate the molecular modeling, structural, and biological properties of these new compounds.

Main Methods:

• Molecular modeling and synthesis of 1,2,3-trisubstituted triazole-Cu(II) complexes.
• Structural characterization using X-ray diffraction, spectroscopy (NMR, IR, UV-Vis), and mass spectrometry.
• In vitro biological assays against Leishmania amazonensis amastigotes and promastigotes.

Main Results:

• Two copper complexes were synthesized and characterized, exhibiting square planar geometry.
• Complex 1 demonstrated significant potency against intracellular amastigotes (IC50 = 0.4 µM), outperforming amphotericin B and pentamidine.
• Complex 1 exhibited a favorable selectivity index (SI = 9.7), indicating potential as a lead compound.

Conclusions:

• Complex 1 is a highly promising candidate for novel antileishmanial drug development.
• The study highlights the therapeutic potential of copper-triazole complexes against leishmaniasis.
• Further in vivo studies are warranted to validate the efficacy of Complex 1.