Chemotherapy based on repeated doses of praziquantel remains the most effective control strategy against schistosomiasis, a neglected tropical disease caused by platyhelminths of the genus Schistosoma spp. Its long‐term use, however, raises serious concerns about drug resistance against praziquantel. Therefore, it is generally acknowledged that alternative treatment options are urgently needed. This Review summarizes data on relinquished drugs as well as recent advances in the area of antischistosomal compounds from a medicinal chemistry point of view. Furthermore, insights into the structure–activity relationships of each class of compounds are presented including in vitro and in vivo data, if available. Although many compounds have demonstrated good antischistosomal activity in vitro, they offer little promise to replace praziquantel. Nevertheless, the race to develop novel antischistosomal agents is ongoing.

中文翻译：

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对抗血吸虫病的化学疗法：过去，现在和未来

基于重复剂量的吡喹酮的化学疗法仍然是针对血吸虫病的最有效的控制策略，血吸虫病是一种由血吸虫属的蠕虫引起的被忽视的热带病。spp。然而，长期使用它引起对吡喹酮耐药性的严重担忧。因此，通常认为迫切需要替代治疗方案。这篇综述从药物化学的角度总结了放弃药物的数据以及抗血吸虫病化合物领域的最新进展。此外，还提供了对每类化合物的结构-活性关系的见解，包括体外和体内数据（如果有）。尽管许多化合物在体外均表现出良好的抗血吸虫病活性，但它们几乎不能替代吡喹酮。尽管如此，开发新型抗血吸虫病药物的竞赛仍在进行中。