Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives

Natália    N.    Santiago; Giulianna    P.    de Alcântara; Juliana    S.   da Costa; Samir    A.    Carvalho; Juliana    M.C.    Barbosa; Kelly       Salomão; Solange    L.    de Castro; Henrique    M.G.    Pereira; Edson    F.    da Silva

doi:10.2174/1573406415666190712115237

Abstract

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.

Keywords: Hydrazonoyl, megazol, nitrofurazone, Chagas' disease, Trypanosoma cruzi, chemotherapy.

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DOI https://dx.doi.org/10.2174/1573406415666190712115237	Print ISSN 1573-4064
Publisher Name Bentham Science Publisher	Online ISSN 1875-6638

Medicinal Chemistry

Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives

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