Department of Organic Chemistry, Faculty of Chemistry, University of Łódź, Tamka 12, 91-403 Łódź, Poland.
M.Sc. Student at the Faculty of Chemistry, University of Łódź, Tamka 12, 91-403 Łódź, Poland.
Molecules. 2017 Jul 7;22(7):1132. doi: 10.3390/molecules22071132.
A wide range of biological activities of aminophosphonates predisposes them to find applications as anticancer, antiviral, antimicrobial, antifungal, or herbicidal agents. Despite a number of positive aspects of the use of aminophosphonates, their applications may cause a risk to the environment, which is well exemplified by the case of glyphosate. Therefore, scientists see a pressing need to rate ecotoxicity of aminophosphonates. Nowadays, it is recommended to use comprehensive tools to carry out appropriate and effective risk assessments of toxic substances. For these purposes, tests based on the acute toxicity of the luminescent bacteria , as well as the measurement of sub-chronic toxicity of the crustacean seem to be the most convenient. A series of five diphenyl -arylamino(pyrrole-2-yl)methylphosphonates was synthesized and preliminary evaluation of their ecotoxicological properties was performed. In order to carry out such investigations, we applied the two biotests mentioned above. Results showed that the -(4-nitrophenyl) derivative was the most toxic for bacteria in comparison to other tested compounds. As for crustaceans, -phenyl and -naphthyl derivatives were found to be the most harmful, simultaneously being relatively harmless for bacteria. Such a phenomenon are discussed in correlation with the literature, while its reason is discussed with respect to the aspect of structure of the tested compounds.
氨基膦酸酯具有广泛的生物活性，这使得它们有望成为抗癌、抗病毒、抗菌、抗真菌或除草剂药物。尽管氨基膦酸酯的使用有许多积极方面，但它们的应用可能会对环境造成风险，草甘膦就是一个很好的例子。因此，科学家们迫切需要评估氨基膦酸酯的生态毒性。如今，建议使用综合工具来对有毒物质进行适当和有效的风险评估。为此，基于发光细菌的急性毒性测试，以及甲壳类动物的亚慢性毒性测量似乎是最方便的。我们合成了一系列五种二苯基-芳基（吡咯-2-基）甲基膦酸酯，并对它们的生态毒性进行了初步评估。为了进行这样的研究，我们应用了上述两种生物测试。结果表明，与其他测试化合物相比，-(4-硝基苯基）衍生物对细菌的毒性最大。对于甲壳类动物，-苯基和-naphthyl 衍生物被发现是最有害的，同时对细菌的危害性相对较小。我们将这种现象与文献进行了讨论，同时还从测试化合物的结构方面讨论了其原因。
