This study investigates cutting-edge synthetic chemistry approaches for designing and producing innovative antimalarial drugs with improved efficacy and fewer adverse effects. Novel amino (–NH) and hydroxy (–OH) functionalized 11-azaartemisinins , , and were synthesized along with their derivatives , , and through ART and were tested for their AMA (antimalarial activity) against via intramuscular () and oral routes in Swiss mice. Ether derivative was the most active compound by route, it has shown 100 % protection at the dose of 12 mg/kg × 4 days and showed 100 % clearance of parasitaemia on day 4 at dose of 6 mg/kg. Amine , ether derivatives , and ether also showed promising antimalarial activity. -Arteether gave 100 % protection at the dose of 48 mg/kg × 4 days and 20 % protection at 24 mg/kg × 4 days dose by oral route, while it showed 100 % protection at 6 mg/kg × 4 days and no protection at 3 mg/kg × 4 days by route.

中文翻译：

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11-氮杂青蒿素的新型醚衍生物对瑞士小鼠的多重耐药约氏疟原虫具有高度抗疟活性

这项研究研究了用于设计和生产创新抗疟药物的尖端合成化学方法，这些药物具有更高的功效和更少的副作用。新型氨基 (–NH) 和羟基 (–OH) 功能化 11-氮杂青蒿素 , , 及其衍生物 , , 和 通过 ART 合成，并在瑞士通过肌内 () 和口服途径测试其 AMA（抗疟活性）老鼠。醚衍生物是最活跃的化合物，在 12 mg/kg × 4 天的剂量下显示出 100% 的保护作用，在 6 mg/kg 的剂量下在第 4 天显示出 100% 的寄生虫血症清除率。胺、醚衍生物和醚也显示出有前景的抗疟活性。 -Arteether 在 48 mg/kg × 4 天剂量下提供 100% 保护，在 24 mg/kg × 4 天口服剂量下提供 20% 保护，而在 6 mg/kg × 4 天剂量下显示 100% 保护，无3 mg/kg × 4 天，途径保护。