Design, Synthesis and Bioactivities of Phenithionate Analogues or Derivatives for Anti-schistosomiasis
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A novel series of phenithionate analogues or derivatives were designed and synthesized using phenithionate as the lead compound, and their bioactivities were studied. Their structures were confirmed by H NMR, C NMR, HR-ESI-MS, and elemental analysis, respectively. The results of inhibitory activity measurement proved that compounds , , , , and had a better inhibitory effect on larva and imago schistosoma. Among them, the inhibitory activity of compound for larva schistosoma was IC = 5.21 ± 0.04 μg mL, and for imago schistosoma it was IC = 6.35 ± 0.08 μg mL. Moreover, the experimental results of anti-schistosomiasis activity measurement showed that they had good anti-schistosomiasis activity. Therefore, these compounds had better drugability.
Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?.
Dziwornu G, Attram H, Gachuhi S, Chibale K RSC Med Chem. 2021; 11(4):455-490.
PMID: 33479649 PMC: 7593896. DOI: 10.1039/d0md00062k.