Schistosomicidal activity of six phthalimido-thiazoles derivatives with substitutions at the position three of the thiazole ring were analyzed in an experimental model. The substituents biphenyl (2i) and 2- naphthyl (2j) at a concentration of 80 µg/mL caused 100% mortality of the parasite in culture after 24 h and 48 h respectively. An evaluation of ultrastructural parasites showed damage in the tegument, formation of bubbles and partial destruction of the tubercles. The in vivo anti-parasitic activity with the derivate 2i was performed by administering it orally and intraperitoneally in a 400 mg/kg/5days regimen. Decreases in the number of eggs in the gut (45.1%) and a reduction of the percentage of mature (23.7%) and increased unviable (53.8%) eggs were observed. Our results also showed a reduction in the number of recovered worms after treatment with 2i (oral administration: 81, 25%). The results demonstrated that the prototypes which were tested had a significant anti-schistosomal effect against S. mansoni, suggesting that these derivatives are promising candidates for further research into the chemotherapy of schistosomiasis.

中文翻译：

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多目标邻苯二甲酰噻唑类药物对曼氏血吸虫的体外和体内活性。

在实验模型中分析了六种在噻唑环的三位被取代的邻苯二甲酰亚胺基噻唑衍生物的血吸虫活性。浓度为80 µg / mL的取代基联苯（2i）和2-萘基（2j）分别在24小时和48小时后导致培养物中寄生虫的100％死亡。对超微结构寄生虫的评估显示其外皮被破坏，气泡形成以及结核的部分破坏。衍生物2i的体内抗寄生虫活性是通过以400mg / kg / 5天的方案口服和腹膜内给药来进行的。观察到肠道中鸡蛋的数量减少了（45.1％），成熟鸡蛋的百分比减少了（23.7％），不活的鸡蛋增加了（53.8％）。我们的结果还显示，用2i治疗后，蠕虫的恢复数量有所减少（口服给药：81％，25％）。结果表明，所测试的原型对曼氏链球菌具有显着的抗血吸虫病作用，表明这些衍生物是有希望用于血吸虫病化学疗法进一步研究的候选者。