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Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives
Medicinal Chemistry ( IF 2.3 ) Pub Date : 2020-05-31 , DOI: 10.2174/1573406415666190712115237
Natália N. Santiago 1 , Giulianna P. de Alcântara 1 , Juliana S. da Costa 1 , Samir A. Carvalho 1 , Juliana M.C. Barbosa 2 , Kelly Salomão 2 , Solange L. de Castro 2 , Henrique M.G. Pereira 3 , Edson F. da Silva 1
Affiliation  

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.



中文翻译:

新型羟基衍生物的合成及抗胰体谱

背景:世界上大约有5-7百万人感染克氏锥虫,每年约有10,000人死于与这种疾病有关的并发症。

方法:这项工作描述了新的Hidrazonoyl取代衍生物家族的结构,在结构上设计了探索兆唑和呋喃西林之间的分子杂交的方法。

结果与讨论:评估了这些化合物对锥虫锥虫血流锥虫的体外活性,查加斯锥虫病的病原体及其对哺乳动物细胞的潜在毒性。

结论:在这些酰基衍生物中,我们鉴定了具有与标准药物Bz相似的锥虫杀虫活性(IC50 / 24 h = 15.0 µM)的衍生物(4),对哺乳动物细胞的毒性低,SI值为18.7。

更新日期:2020-05-31
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