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新型含氮化合物与酚类单元的偶联物具有抗氧化和抗真菌活性:合成及结构-活性关系。

New Nitrogen Compounds Coupled to Phenolic Units with Antioxidant and Antifungal Activities: Synthesis and Structure⁻Activity Relationship.

机构信息

Department of Chemistry, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal.

Department of Pharmacology, Center for Research in Molecular Medicine and Chronic Diseases (CiMUS), Universidade de Santiago de Compostela, Avenida de Barcelona 22, 15782 Santiago de Compostela, Spain.

出版信息

Molecules. 2018 Oct 3;23(10):2530. doi: 10.3390/molecules23102530.

Abstract

A selection of 1-amino-2-arylidenamine-1,2-(dicyano)ethenes was synthesized and cyclized to 2-aryl-4,5-dicyano-1-imidazoles upon reflux in ethyl acetate/acetonitrile, in the presence of manganese dioxide. These compounds were tested for their antioxidant capacity by cyclic voltammetry, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and deoxyribose degradation assays. The minimum inhibitory concentration of all compounds was evaluated against two yeast species, and . Their toxicity was tested in mammal fibroblasts. Among the synthesised compounds, two presented dual antioxidant/antifungal activity without toxic effects in fibroblasts. The new compounds synthesized in this work are potential biochemical tools and/or therapeutic drugs.

摘要

选择了一系列 1-氨基-2-芳基亚氨基-1,2-(二氰基)乙烯,并在乙酸乙酯/乙腈回流的条件下,在二氧化锰的存在下环化成 2-芳基-4,5-二氰基-1-咪唑。通过循环伏安法、2,2-二苯基-1-苦基肼(DPPH)自由基和脱氧核糖降解测定法,测试了这些化合物的抗氧化能力。用两种酵母,和,评估了所有化合物的最小抑菌浓度。在哺乳动物成纤维细胞中测试了它们的毒性。在所合成的化合物中,有两种表现出双重抗氧化/抗真菌活性,且对成纤维细胞没有毒性作用。本工作中合成的新化合物是潜在的生化工具和/或治疗药物。

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