Department of Organic Chemistry, Medical University, Chodźki 4a, 20-093 Lublin, Poland.
Department of Immunoparasitology, Faculty of Biology and Environmental Protection, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland.
Molecules. 2019 Feb 10;24(3):614. doi: 10.3390/molecules24030614.
One of the key stages in the development of new therapies in the treatment of toxoplasmosis is the identification of new non-toxic small molecules with high specificity to . In the search for such structures, thiosemicarbazide-based compounds have emerged as a novel and promising leads. Here, a series of imidazole-thiosemicarbazides with suitable properties for CNS penetration was evaluated to determine the structural requirements needed for potent anti- activity. The best 4-arylthiosemicarbazides and showed much higher potency when compared to sulfadiazine at concentrations that are non-toxic to the host cells, indicating a high selectivity of their anti-toxoplasma activity.
在开发治疗弓形虫病的新疗法的过程中,关键阶段之一是确定具有高特异性的新型无毒小分子。在寻找此类结构的过程中,基于硫代卡巴肼的化合物已成为一种新颖且有前途的先导化合物。在这里,评估了一系列具有适合 CNS 穿透特性的咪唑硫代卡巴肼,以确定具有有效抗弓形虫活性所需的结构要求。与磺胺嘧啶相比,最佳的 4-芳基硫代卡巴肼 和 具有更高的效力,而在对宿主细胞无毒的浓度下,表明其抗弓形虫活性具有很高的选择性。