Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives

Author(s): 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*

Journal Name: Medicinal Chemistry

Volume 16 , Issue 4 , 2020

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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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VOLUME: 16
ISSUE: 4
Year: 2020
Published on: 21 May, 2020
Page: [487 - 494]
Pages: 8
DOI: 10.2174/1573406415666190712115237
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