Malaria, a devastating disease, has claimed numerous lives and caused considerable suffering, with young children and pregnant women being the most severely affected group. However, the emergence of multidrug-resistant strains of and the adverse side effects associated with existing antimalarial drugs underscore the urgent need for the development of novel, well-tolerated, and more efficient drugs to combat this global health threat. To address these challenges, six new hydantoins derivatives were synthesized and evaluated for their antiplasmodial activity. Notably, compound exhibited excellent inhibitory activity against the tested 3D7 strain, with an IC value of 3.97 ± 0.01 nM, three-fold better than chloroquine. Following closely, compound demonstrated an IC value of 27.52 ± 3.37 µM against the 3D7 strain . Additionally, all the hydantoins derivatives tested showed inactive against human MCR-5 cells, with an IC value exceeding 100 μM. In summary, the hydantoin derivative emerges as a promising candidate for further exploration as an antiplasmodial compound.

中文翻译：

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乙内酰脲衍生物作为有效抗疟原虫剂的合成和生物学评价

疟疾是一种毁灭性的疾病，夺去了无数人的生命，造成了巨大的痛苦，其中幼儿和孕妇是受影响最严重的群体。然而，多重耐药菌株的出现以及与现有抗疟药物相关的不良副作用强调迫切需要开发新型、耐受性良好且更有效的药物来应对这一全球健康威胁。为了应对这些挑战，合成了六种新的乙内酰脲衍生物并评估了它们的抗疟原虫活性。值得注意的是，该化合物对测试的 3D7 菌株表现出优异的抑制活性，IC 值为 3.97 ± 0.01 nM，是氯喹的三倍。紧随其后，化合物对 3D7 菌株的 IC 值为 27.52 ± 3.37 µM。此外，所有测试的乙内酰脲衍生物均对人 MCR-5 细胞无活性，IC 值超过 100 μM。总之，乙内酰脲衍生物作为抗疟原虫化合物作为进一步探索的有希望的候选者。