Diglycosyl diselenides alter redox homeostasis and glucose consumption of infective African trypanosomes

With the aim to develop compounds able to target multiple metabolic pathways and, thus, to lower the chances of drug resistance, we investigated the anti-trypanosomal activity and selectivity of a series of symmetric diglycosyl diselenides and disulfides. Of 18 compounds tested the fully acetylated...

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Bibliographic Details
Published in:International journal for parasitology -- drugs and drug resistance 2017-12, Vol.7 (3), p.303-313
Main Authors: Franco, Jaime, Sardi, Florencia, Szilágyi, László, Kövér, Katalin E., Fehér, Krisztina, Comini, Marcelo A.
Format: Article
Language:English
Subjects:
Glutathione
Redox biosensor
Selenium NMR
Selenosugar
Trypanosome inhibition
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Summary:With the aim to develop compounds able to target multiple metabolic pathways and, thus, to lower the chances of drug resistance, we investigated the anti-trypanosomal activity and selectivity of a series of symmetric diglycosyl diselenides and disulfides. Of 18 compounds tested the fully acetylated forms of di-β-D-glucopyranosyl and di-β-D-galactopyranosyl diselenides (13 and 15, respectively) displayed strong growth inhibition against the bloodstream stage of African trypanosomes (EC50 0.54 μM for 13 and 1.49 μM for 15) although with rather low selectivity (SI 
ISSN:2211-3207
2211-3207
DOI:10.1016/j.ijpddr.2017.08.001