Exploring Quinazoline Nitro-Derivatives as Potential Antichagasic Agents: Synthesis and In Vitro Evaluation

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Abstract
Trypanosoma cruzi is a protozoan parasite that causes Chagas disease in humans. The current antichagasic drugs nifurtimox and benznidazole have inconveniences of toxicity; therefore, the search for alternative therapeutic strategies is necessary. The present study reports the synthesis, drug-likeness predictions, and in vitro anti-trypanosome activity of a series of 14 quinazoline 2,4,6-triamine derivatives. All compounds were tested against T. cruzi (epimastigotes and trypomastigotes) and in HFF1 human foreskin fibroblasts. The bioassays showed that compounds 2–4 containing nitrobenzoyl substituents at 6-position of the quinazoline 2,4,6-triamine nucleus were the most potent on its antiprotozoal activity. The effect was observed at 24 h and it was preserved for at least 5 days. Also, compounds 2–4 were not toxic to the human control cells, showing high selectivity index. The quinazoline nitro derivatives have potential use as antichagasic agents.
Funding Information
  • Secretaría de Ciencia, Humanidades, Tecnología e Innovación (264292, 272941, 282663, CBF-2023-2024-2740)
  • Secretaría de Ciencia, Humanidades, Tecnología e Innovación (264292, 272941, 282663, CBF-2023-2024-2740)
  • Secretaría de Ciencia, Humanidades, Tecnología e Innovación (264292, 272941, 282663, CBF-2023-2024-2740)
  • Secretaría de Ciencia, Humanidades, Tecnología e Innovación (264292, 272941, 282663, CBF-2023-2024-2740)

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