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Hybrid Compounds Strategy in the Synthesis of Oleanolic Acid Skeleton-NSAID Derivatives

机译:齐墩果酸骨架-NSAID衍生物合成中的杂化化合物策略

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摘要

The current study focuses on the synthesis of several hybrid individuals combining a natural oleanolic acid skeleton and synthetic nonsteroidal anti-inflammatory drug moieties (NSAIDs). It studied structural modifications of the oleanolic acid structure by use of the direct reactivity of hydroxyl or hydroxyimino groups at position C-3 of the triterpenoid skeleton with the carboxylic function of anti-inflammatory drugs leading to new perspective compounds with high potential pharmacological activities. Novel ester- and iminoester-type derivatives of oleanolic unit with the different NSAIDs, such as ibuprofen, aspirin, naproxen, and ketoprofen, were obtained and characterized. Moreover, preliminary research of compounds obtaining structure stability under acidic conditions was examined and the PASS method of prediction of activity spectra for substances was used to estimate the potential biological activity of these compounds.
机译:当前的研究集中在几个杂种个体的合成上,这些个体结合了天然齐墩果酸骨架和合成的非甾体抗炎药部分(NSAIDs)。通过利用三萜类骨架的C-3位上的羟基或羟基亚氨基的直接反应性与抗炎药的羧基功能,研究了齐墩果酸结构的结构修饰,从而开发出具有高潜在药理活性的新型观点化合物。获得并鉴定了具有不同NSAID的齐墩果酸单元的新型酯和亚氨基酯型衍生物,并对其进行了表征。此外,对化合物在酸性条件下获得结构稳定性的初步研究进行了审查,并使用PASS方法预测物质的活性谱来估计这些化合物的潜在生物活性。

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