Pachuta-Stec Anna, Nowak Renata, Pietrzak Wioleta, Pitucha Monika
Independent Radiopharmacy Unit, Faculty of Pharmacy with Medical Analytics Division, Medical University of Lublin, 4 A Chodźki Street, PL-20-093, Lublin, Poland.
Department of Pharmaceutical Botany, Faculty of Pharmacy with Medical Analytics Division, Medical University of Lublin, 1 Chodźki Street, PL-20-093, Lublin, Poland.
Chem Biodivers. 2019 Apr;16(4):e1800673. doi: 10.1002/cbdv.201800673. Epub 2019 Mar 19.
New norcantharidin analogs were designed and obtained as compounds with biological activity. As a starting material, exo-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid anhydride was used. Three groups of compounds: dicarboximides, triazoles and thiazolidines were obtained in multistep reactions. The H- and C-NMR spectra were used to confirm the structures of all obtained products and they were in agreement with the proposed structure of substances. All derivatives were screened for their antioxidant activity. The most promising group was dicarboximides (1-4, 6). Derivatives 2-4 displayed antioxidant activity with EC =7.75-10.89 μg/ml, which may be comparable to strong antioxidant Trolox (EC =6.13 μg/ml). Excellent activity with EC =10.75 μg/ml also presented norcantharidin analog with 1,2,4-triazole system (12).
设计并获得了具有生物活性的新型去甲斑蝥素类似物。以外向-7-氧杂双环[2.2.1]庚烷-2,3-二羧酸酐为起始原料。通过多步反应得到了三组化合物：二羧酰亚胺、三唑和噻唑烷。利用氢核磁共振谱和碳核磁共振谱确认了所有所得产物的结构，它们与所提出的物质结构一致。对所有衍生物进行了抗氧化活性筛选。最有前景的一组是二羧酰亚胺（1-4, 6）。衍生物2-4表现出抗氧化活性，其半数有效浓度（EC）为7.75-10.89μg/ml，这可能与强抗氧化剂Trolox（EC =6.13μg/ml）相当。具有1,2,4-三唑体系的去甲斑蝥素类似物（12）也表现出优异的活性，其半数有效浓度（EC）为10.75μg/ml。
