吡嗪取代1,3,4-噻二唑衍生物的合成及其抗惊厥活性

K. Harish, K. Mohana, L. Mallesha
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引用次数: 9

摘要

以吡嗪取代的1,3,4-噻二唑为原料,与各种磺酰氯反应,合成了新的吡嗪取代的1,3,4-噻二唑衍生物,收率较高。所有新化合物的化学结构都通过1H NMR和质谱数据得到了证实。新化合物对最大电休克(MES)发作法的抗惊厥活性进行了筛选。采用轮棒法测定神经毒性。很少有化合物在抗惊厥活性方面表现出显著的变化。相同的化合物在最大剂量(100 mg/kg)下没有神经毒性。
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Synthesis of Pyrazine Substituted 1,3,4-Thiadiazole Derivatives and Their Anticonvulsant Activity
The synthesis of new pyrazine substituted 1,3,4-thiadiazole derivatives was carried out in good yield by the reaction of pyrazine substituted 1,3,4-thiadiazoles with various sulfonyl chlorides. A chemical structure of all the new compounds was confirmed by 1H NMR and mass spectral data. The new compounds were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method. Rotarod method was employed to determine the neurotoxicity. Few compounds showed significant changes in anticonvulsant activity. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg).
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