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

Abstract

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.