LASOL-CCQFA, Universidade Federal de Pelotas - UFPel, P.O. Box 354, 96010-900, Pelotas, RS, Brazil.
Neurobiotechnology Research Group - GPN, Technological Development Center, Federal University of Pelotas - UFPel, Pelotas, RS, 96160-000, Brazil.
Chem Asian J. 2024 Oct 1;19(19):e202400637. doi: 10.1002/asia.202400637. Epub 2024 Sep 3.
We present our results on the synthesis and preliminary in silico and in vitro studies of the toxicology and antioxidant properties of selenylated analogs of Tacrine. Initially, we synthesized 2-aminobenzonitriles containing an organic selenium moiety, resulting in sixteen compounds with various substituents linked to the portion derived from diorganyl diselenide. These compounds were then used as substrates in reactions with cyclic ketones, in the presence of 1.4 equivalents of trifluoroboroetherate as a Lewis acid, to synthesize selenylated analogs of Tacrine with yields ranging from 20 % to 87 %. In silico studies explored computational parameters related to antioxidant activity and hepatotoxicity. In vitro studies elucidated the antioxidant effects of Tacrine and its selenium hybrid (TSe) in neutralizing ABTS radicals, scavenging DPPH radicals, and reducing iron ions. Additionally, the acute oral toxicity of one synthesized compound was evaluated.
我们介绍了我们在合成和初步的毒理学和抗氧化性质的模拟物以及 Tacrine 的体内研究方面的结果。最初,我们合成了含有有机硒部分的 2-氨基苯甲腈,得到了十六个化合物,它们具有不同的取代基与二有机二硒化物衍生的部分相连。然后,在路易斯酸 1.4 当量的三氟硼酸酯存在下,将这些化合物用作与环状酮的反应的底物,以 20%至 87%的产率合成 Tacrine 的硒代类似物。体内研究探讨了与抗氧化活性和肝毒性相关的计算参数。体外研究阐明了 Tacrine 及其硒杂化物(TSe)在中和 ABTS 自由基、清除 DPPH 自由基和还原铁离子方面的抗氧化作用。此外,还评估了一种合成化合物的急性口服毒性。