Oxadiazole-2-oxides may have other functional targets, in addition to SjTGR, through which they cause mortality in Schistosoma japonicum

Parasites & Vectors
Li-Jun SongChuan-Xin Yu

Abstract

Schistosomiasis is one of the world's major public health problems. Besides praziquantel (PZQ), there is currently no other effective treatment against schistosomiasis. The development of new antischistosomal agents to curb the emergence of PZQ resistance should be a high priority. Oxadiazole-2-oxides have been identified as potential antischistosomal reagents, with thioredoxin glutathione reductase (TGR) being one of their molecular targets. To develop novel treatment reagents against Schistosoma japonicum, 30 novel oxadiazole-2-oxides were synthesised and their antischistosomal activities on juvenile and adult S. japonicum were evaluated in vitro and in vivo. Their inhibitory activities against S. japonicum thioredoxin glutathione reductase (SjTGR) were also analysed. Most of the oxadiazole-2-oxides showed good juvenile and adult S. japonica killing activities in vitro. However, the antischistosomal effects of these compounds were not positively correlated with either their inhibition of SjTGR, or with nitric oxide (NO) release. Compounds 4a, 4b, 7c, 13, 16 and 20 resulted in 87.7%, 83.1%, 87.1%, 84.6%, 90.8% and 69.5%, respectively, mortality in the adult worms, when used to treat infected mice at schistosomula stage. These ...Continue Reading

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Citations

Dec 14, 2017·Future Medicinal Chemistry·Eloi M LagoJosué de Moraes
Sep 14, 2018·ChemMedChem·Patrick MäderMartin Schlitzer
Apr 4, 2021·Pathogens·Viatcheslav A MordvinovMaria Y Pakharukova
Jan 26, 2018·Chemico-biological Interactions·Luana Maria Mariz Gomes da SilvaMonica Camelo Pessoa de Azevedo Albuquerque

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