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首页> 外文期刊>Brazilian Journal of Pharmaceutical Sciences >Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents
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Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents

机译：邻硝基苄基衍生物可作为潜在的抗血吸虫病药物

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In the search for new anti-schistosomal agents, a series of fifteen ortho -nitrobenzyl derivatives was assayed in vitro against both the schistosomulum (somule) and adult forms of Schistosoma mansoni . Compounds 8 and 12 showed significant activity against somules at low micromolar concentrations, but none was active against adults. The SAR demonstrated that the compounds most active against the parasite were mutagenic to the human cell line RKO-AS45-1 only at concentrations 10- to 40-fold higher than the worm-killing dose. Given their electrophilicity, compounds were also screened as inhibitors of the S. mansoni cysteine protease (cathepsin B1) in vitro . Amides 5 and 15 exhibited a modest inhibition activity with values of 55.7 and 50.6 % at 100 μM, respectively. The nitrobenzyl compounds evaluated in this work can be regarded as hits in the search for more active and safe anti-schistosomal agents.
机译：在寻找新的抗血吸虫病药物时，在体外针对曼氏血吸虫的血吸虫病（配伍）和成年形式对了十五种邻硝基苄基衍生物进行了分析。化合物8和12在低微摩尔浓度下显示出显着的抗肌动蛋白活性，但对成年人没有活性。 SAR表明，对寄生虫最具活性的化合物对人细胞系RKO-AS45-1的诱变作用仅比杀虫剂量高10至40倍。考虑到它们的亲电性，化合物在体外也被筛选为曼氏葡萄球菌半胱氨酸蛋白酶（cathepsin B1）的抑制剂。酰胺5和15在100μM时表现出适度的抑制活性，分别为55.7和50.6％。在这项工作中评估的硝基苄基化合物可被视为寻找更有效，更安全的抗血吸虫病药物的热门产品。

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