Nifurtimox is a nitrofurane derivative antiprotozoal that shows anti Trypanosoma cruzi activity through bioreduction of the nitro-group and dependence on redox cycling with O2. When used in combination with Buthionine Sulfoximine (sc-200824), Nifurtimox has displayed increased toxicity toward the epimastigote, trypomastigote, and amastigote forms of Trypanosoma cruzi. In the mammary tissue of female Sprague-Dawley rats Nifurtimox was observed, in a purine dependent manner, to biotransform to xanthine-oxioreductase in the cytosol. This activity can be inhibited by Allopurinol (sc-207272). The compound has also gone under the same transformation in the presence of NADPH and inhibited partially by Diphenyleneiodonium chloride (sc-202584) and completely by carbon monoxide.
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