Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives
作者:Zahra Abada、Sandrine Cojean、Sébastien Pomel、Laurent Ferrié、Bernardin Akagah、Anh Tuan Lormier、Philippe M. Loiseau、Bruno Figadère
DOI:10.1016/j.ejmech.2013.06.002
日期:2013.9
potential of porphyrins and their precursors and derivatives as potential antiparasitic agents by interfering with heme metabolism. Consequently, twenty-four porphyrin precursors and derivatives were evaluated against Leishmania donovani, Trypanosoma brucei and Plasmodium sp. The best active compound against Trypanosoma brucei brucei was a new porphyrin derivative; compound 4i, with a MEC value of 6.25 μM
血红素在非洲锥虫Leishmania sp。中的重要性。和疟原虫属。代谢证明通过干扰血红素代谢来考虑卟啉及其前体和衍生物作为潜在抗寄生虫剂的潜力。因此,评估了二十四种卟啉前体和衍生物对利什曼原虫,布鲁氏锥虫和疟原虫。对抗布鲁氏锥虫的最佳活性化合物是一种新的卟啉衍生物。化合物4i的MEC值为6.25μM,证明在体内有进一步的应用评估。而这些化合物并不反对的无鞭毛体intramacrophage活性大号。 donovani,另一种新的卟啉衍生物,化合物4f在20 nM时具有体外抗恶性疟原虫活性,在伯氏疟原虫/ Swiss小鼠模型中观察到小鼠存活略有延迟,浓度为50μmol/ kg /天×4。依赖于对卟啉行为的更好了解而开发的寄主相对于宿主细胞而言。