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Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives
Natália N Santiago1,2, Giulianna P de Alcântara1,2, Juliana S da Costa1,3
1Instituto de Tecnologia em Farmacos, Farmanguinhos, Laboratorio de sintese 1, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Brazil.
Background:
Approximately, 5-7 million people are infected with T. cruzi in the world, and approximately 10,000 people per year die of complications linked to this disease.
Methods:
This work describes the construction of a new family of hidrazonoyl substituted derivatives, structurally designed exploring the molecular hybridization between megazol and nitrofurazone.
Results And Discussion:
The compounds were evaluated for their in vitro activity against bloodstream trypomastigotes of Trypanosoma cruzi, etiological agent of Chagas disease, and for their potential toxicity to mammalian cells.
Conclusion:
Among these hydrazonoyl derivatives, we identified the derivative (4) that showed trypanocidal activity (IC50/24 h = 15.0 µM) similar to Bz, the standard drug, and low toxicity to mammalian cells, reaching an SI value of 18.7.
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