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首页> 外文期刊>Arzneimittel-Forschung: =Drug Research >Synthesis and anticonvulsant activity of new kojic acid derivatives.
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Synthesis and anticonvulsant activity of new kojic acid derivatives.

机译：新曲酸衍生物的合成及其抗惊厥活性。

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摘要

A series of new 3-hydroxy-6-hydroxymethyl-2-substituted 4H-pyran-4-one derivatives were synthesized as potential anticonvulsant compounds. Mannich compounds were prepared by the reaction of appropriate substituted piperazine derivatives with kojic acid and formaline. The structure of the synthesized compounds was confirmed using the elementary analysis results and spectroscopic techniques such as IR, 1H-NMR and ESI-MS. Anticonvulsant activities of the synthesized compounds were examined by maximal electroshock (MES) and subcutaneous Metrazol (scMet) induced seizure tests. Neurotoxicity was determined by the rotorod toxicity test. All these tests were performed according to procedures of the Antiepileptic Drug Development (ADD) program. According to the activity studies, 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]-3-hydroxy-6-hydroxymethyl-4H-pyran-4-o ne (compound 11) against MES seizures and 3-hydroxy-6-hydroxymethyl-2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]-4H-pyran-4- one (compound 7) against scMet seizures were determined to be the most active compounds at all doses without neurotoxicity.
机译：合成了一系列新的3-羟基-6-羟甲基-2-取代的4H-吡喃-4-酮衍生物，作为潜在的抗惊厥化合物。通过合适的取代的哌嗪衍生物与曲酸和福尔马林的反应制备曼尼希化合物。使用元素分析结果和光谱技术（例如IR，1H-NMR和ESI-MS）确认了合成化合物的结构。通过最大电休克（MES）和皮下美曲唑（scMet）诱发的癫痫发作试验检查了合成化合物的抗惊厥活性。神经毒性由旋翼毒性试验确定。所有这些测试均根据抗癫痫药物开发（ADD）程序进行。根据活性研究，2- [4-（4-氯苯基）哌嗪-1-基甲基] -3-羟基-6-羟基甲基-4H-吡喃-4-烯（化合物11）对抗MES发作和3-羟基确定抗scMet癫痫发作的-6-羟甲基-2- [4-（2-甲氧基苯基）哌嗪-1-基甲基] -4H-吡喃-4-酮（化合物7）是所有剂量下活性最高的化合物，无神经毒性。

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