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Chemotherapy for Fighting Schistosomiasis: Past, Present and Future

机译:用于战斗血吸虫病的化疗:过去,现在和未来

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摘要

Chemotherapy based on repeated doses of praziquantel remains the most effective control strategy against schistosomia-sis, 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.
机译:基于重复剂量的吡喹酮的化疗仍然是对血吸虫-SIS的最有效的控制策略,这是由血吸虫属Platyhelminth引起的被忽略的热带病。 然而,它的长期使用引起了对吡喹酮的耐药性的严重担忧。 因此,通常承认迫切需要替代治疗方案。 本综述总结了对放牧药物的数据以及来自药物化学的抗血栓药物化合物领域的最新进展。 此外,如果有的话,介绍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。 虽然许多化合物在体外证明了良好的反痉挛活性,但它们提供了替代吡喹酮的许多承诺。 尽管如此,开发新型抗脱肌腱药物的种族正在进行中。

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