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首页> 外文期刊>Archiv der Pharmazie >Anticonvulsant and Neurotoxicity Evaluation of Some Novel Kojic Acids and Allomaltol Derivatives
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Anticonvulsant and Neurotoxicity Evaluation of Some Novel Kojic Acids and Allomaltol Derivatives

机译：某些新型曲酸和异麦芽酚衍生物的抗惊厥和神经毒性评价

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A series of new 3-hydroxy-6-hydroxymethyl/methyl-2-substituted 4H-pyran-4-ones were synthesized and prepared by the reaction of kojic acid or allomaltol with piperidine derivatives and formaline as potential anticonvulsant compounds. The structure of the synthesized compounds was confirmed using the elemental analysis results and the spectroscopic techniques such as IR, 1H-NMR, and ESI-MS. Anticonvulsant activities 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 in accordance with the procedures of the Antiepileptic Drug Development (ADD) program. According to the activity studies and at all doses, 3-hydroxy-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-6-methyl-4H-pyran-4-one (compound 1), 2-{[4-(4-chlorophenyl)-3,6-dihydropyridin-1(2H)-yl]methyl}-3-hydroxy-6-methyl-4H-pyran-4-one (compound 6), 2-[(4-acetyl-4-phenylpiperidin-1-yl)methyl]-3-hydroxy-6-(hydroxymethyl)-4H-pyran-4-one (compound 11), and 2-{[4-(4-chlorophenyl)-3,6-dihydropyridin-1(2H)-yl] methyl}-3-hydroxy-6-hydroxymethyl-4H-pyran-4-one (compound 12) were found to have anticonvulsant activity against MES-induced seizures at 4 h. Also, 2-{[4-(4-bromophenyl)-4-hydroxypiperidin-1-yl]methyl}-3-hydroxy-6-(hydroxymethyl)-4H-pyran-4-one (compound 8) was determined to be the most active compound against scMet-induced seizures at all doses at 0.5 and 4 h. In the rotorod neurotoxicity screening, all compounds showed no toxicity at all doses.
机译：通过曲酸或异麦芽酚与哌啶衍生物和福尔马林作为潜在的抗惊厥化合物反应，合成并制备了一系列新的3-羟基-6-羟甲基/甲基-2-取代的4H-吡喃-4-酮。使用元素分析结果和IR， 1 H-NMR和ESI-MS等光谱技术确定了合成化合物的结构。通过最大电休克（MES）和皮下美曲唑（scMet）诱导的癫痫发作检查抗惊厥活性。神经毒性由旋翼毒性试验确定。所有这些测试均按照抗癫痫药物开发（ADD）程序的程序进行。根据活性研究和所有剂量，3-羟基-2-[（4-羟基-4-苯基哌啶-1-基）甲基] -6-甲基-4H-吡喃-4-酮（化合物1），2 -{[[4-（4-氯苯基）-3,6-二氢吡啶-1-1（2H）-基]甲基} -3-羟基-6-甲基-4H-吡喃-4-酮（化合物6），2- [ （4-乙酰基-4-苯基哌啶-1-基）甲基] -3-羟基-6-（羟甲基）-4H-吡喃-4-酮（化合物11）和2-{[4-（4-氯苯基） -3,6-二氢吡啶-1（2H）-基]甲基} -3-羟基-6-羟甲基-4H-吡喃-4-酮（化合物12）在4 h对MES诱发的癫痫发作具有抗惊厥活性。另外，确定2-{[4-（4-溴苯基）-4-羟基哌啶-1-基]甲基} -3-羟基-6-（羟甲基）-4H-吡喃-4-酮（化合物8）为在0.5和4小时所有剂量下，对scMet诱发的癫痫发作最有活性的化合物。在旋梭神经毒性筛选中，所有化合物在所有剂量下均无毒性。

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