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Med Chem ; 16(4): 487-494, 2020.
Article in English | MEDLINE | ID: mdl-31309899

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.


Subject(s)
Hydrazones/chemical synthesis , Hydrazones/pharmacology , Trypanocidal Agents/chemical synthesis , Trypanocidal Agents/pharmacology , Trypanosoma cruzi/drug effects , Animals , Cell Line , Chemistry Techniques, Synthetic , Hydrazones/chemistry , Structure-Activity Relationship , Trypanocidal Agents/chemistry
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