Abstract A series of 2-substituted vinylidene-1,1-bisphosphonate esters and their acids were synthesized and tested in vitro for activity against Plasmodium falciparum and Trypanosoma brucei. For each compound, % parasite viability in treated wells was calculated relative to untreated controls for both P. falciparum and T. brucei. Fifty percentage inhibitory concentration (IC50) was also determined for the compounds. Chloroquine and pentamidine were used as positive control drug standards for activity against P. falciparum and T. brucei, respectively. The esters had better antiparasitic activity compared to their corresponding acids. Some of the compounds reduced % parasite viability to as low as 24.3% for P. falciparum and down to 0.602% for T. brucei. Tetraethyl-2-(o-tolyl)-ethene-1,1-bisphosphonate (3b) recorded the best IC50 against T. brucei which was 0.0345 µmol/mL. GRAPHICAL ABSTRACT

中文翻译：

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2-取代乙烯基双膦酸盐对恶性疟原虫和布氏锥虫的合成和生物学评价

摘要 合成了一系列 2-取代的亚乙烯基-1,1-二膦酸酯及其酸，并在体外测试了它们对恶性疟原虫和布氏锥虫的活性。对于每种化合物，相对于恶性疟原虫和布氏锥虫的未处理对照计算处理孔中寄生虫存活率百分比。还测定了化合物的 50% 抑制浓度 (IC50)。氯喹和喷他脒分别用作抗恶性疟原虫和布氏锥虫活性的阳性对照药物标准品。与其相应的酸相比，酯具有更好的抗寄生虫活性。一些化合物将恶性疟原虫的寄生虫存活率降低至 24.3%，将布氏锥虫降低至 0.602%。Tetraethyl-2-(o-tolyl)-ethene-1,1-bisphosphonate (3b) 记录了对 T 的最佳 IC50。布鲁氏菌浓度为 0.0345 µmol/mL。图形概要