Structural optimization of 3-hydroxy-N′-arylidenepropanehydrazonamides provided new analogs with nanomolar to subnanomolar antiplasmodial activity against asexual blood stages of Plasmodium falciparum, excellent parasite selectivity, and nanomolar activity against the earliest forms of gametocyte development. Particularly, derivatives with a 1,3-dihalo-6-trifluoromethylphenanthrene moiety showed outstanding in vivo properties and demonstrated in part curative activity in the Plasmodium berghei mouse model when administered perorally.

中文翻译：

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3-羟基- ñ '与卤素取代的菲支架固化-arylidenepropanehydrazonamides伯氏疟原虫感染小鼠口服给药时

结构优化的3-羟基-N'-亚芳基丙肼酰胺提供了新的类似物，其对恶性疟原虫的无性血液阶段具有纳摩尔至亚纳摩尔的抗血浆活性，具有极佳的寄生虫选择性，并且具有针对最早形式的配子细胞发育的纳摩尔活性。特别地，当口服给予时，具有1，3-二卤代-6-三氟甲基菲部分的衍生物在伯氏疟原虫小鼠模型中显示出优异的体内特性，并在部分治疗活性中得到证明。