Copper(II) complexes with 2-pyridyl-quinazoline ligands with potential activity for Chagas disease treatment

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Abstract

Chagas disease is classified as a neglected tropical disease, caused by the parasite Trypanosoma cruzi, it still lacks effective treatment. In this context, the present study aimed to synthesize and characterize a series of 2-pyridyl-quinazoline ligands with chlorine, fluorine, methyl, and hydrogen substituents and the respective copper(II) mononuclear coordination compounds. The complexes contains a 2-pyridyl-quinazoline ligand unit coordinated to copper(II) through a chelate ring and two chloride ions. The compounds showed trypanocidal activity against the trypomastigote form consistent with literature data for organic compounds and copper(II) complexes – the quinazolyl derivatives exhibited half-maximal inhibitory concentration (IC50) values between 2.43 and 0.23 μmol L-1 and the complexes between 0.43 and 0.14 μmol L-1. For the amastigote morphology, only the series of complexes was evaluated, with fluorine showing the most promising result, with an IC50 of 0.32 μmol L-1. Cytotoxicity tests showed that the complexes are less selective than the ligands.

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Institutions
  • 1 Universidade do Estado do Rio de Janeiro
Track
  • TL03 - Biological and Medicinal Inorganic Chemistry
Keywords
Chagas disease
Coordination compounds
Copper(II)
Amastigote
Trypomastigote