Design, synthesis and bioactivities of phenithionate analogues or derivatives for anti-schistosomiasis.

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 1H NMR, 13C NMR, HR-ESI-MS, and elemental analysis, respectively. The results of in vitro inhibitory activity measurement proved that compounds 5a, 5c, 5g, 5i, 5m and 5o had a better inhibitory effect on larva and imago schistosoma. Among them, the inhibitory activity of compound 5i for larva schistosoma was IC50 = 5.21 ± 0.04 μg mL-1, and for imago schistosoma it was IC50 = 6.35 ± 0.08 μg mL-1. Moreover, the experimental results of in vivo anti-schistosomiasis activity measurement showed that they had good anti-schistosomiasis activity. Therefore, these compounds had better drugability.