A nitrofuran antibiotic
Nitrofurazone (NFZ;Nitrofural) is a bactericidal compound used as an antibiotic most commonly in the form of ointments.Target: AntibacterialNitrofurazone (NFZ;Nitrofural), a nitroaromatic drug, is a broad spectrum antibiotic which has until now been considered as activated in bacteria by nitroreductases. Its use in medicine has become less frequent as safer and more effective products have become available, and it has been discontinued in the US.Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. In vitro cruzain inhibition tests were performed for both compounds, and the 50% inhibitory concentration (IC50) for NF and NFOH presented values of 22.83 ± 1.2 μM and 10.55 ± 0.81 μM, respectively. AM1 semi-empirical molecular modeling studies were performed to understand the activity of the compounds, corroborating the observed cruzain inhibitory activity.
参考文献:
[1]. Ryan A, et al. Activation of nitrofurazone by azoreductases: multiple activities in one enzyme. Sci Rep. 2011;1:63.
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