Synthesis of N-acetyl and N-formyl pyrazoline derivatives from vanillin and their antigenotoxic activity

Jovana Muskinja, S. Matić, S. Stanić, Z. Ratković
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Abstract

: Vanillin is one of the most important natural products, used as a starting material in the new drug design procedures. Starting from vanillin, we can prepare different chalcones, which are known for their pronounced pharmacological and biological activities. For this reason some chalcone analogues have been synthesized from the corresponding vanillin derivatives. Further reaction with hydrazine in formic acid or acetic acid yielded 20 new pyrazoline compounds with N -formyl and N -acetyl groups, respectively. All new compounds were well characterized by IR, 1 H and 13 C NMR spectroscopy and physical data. In vitro DNA protective potential of selected compounds on hydroxyl and peroxyl radical-induced DNA damage was investigated. The results showed that the new synthesized compounds had expressed potential to prevent DNA damage.
香兰素n -乙酰基和n -甲酰基吡唑啉衍生物的合成及其抗毒活性
香兰素是最重要的天然产物之一,在新药设计过程中用作起始原料。从香兰素开始,我们可以制备不同的查尔酮,这些查尔酮以其显著的药理和生物活性而闻名。因此,从相应的香兰素衍生物合成了一些查尔酮类似物。进一步与肼在甲酸或乙酸中反应,分别得到20个新的N -甲酰基和N -乙酰基吡唑啉化合物。所有新化合物均通过IR、1h、13c NMR和物理数据进行了表征。研究了所选化合物对羟基和过氧自由基诱导的DNA损伤的体外保护作用。结果表明,新合成的化合物具有防止DNA损伤的潜力。
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