Previous studies on the anticonvulsant activity of N-Cbz-alpha-aminoglutarimides have shown that the derivatives of N-Cbz-alpha-amino-N-alkoxy glutarimide have significant anticonvulsant activity. In addition, their anticonvulsant activities are dependent on the presence of N-alkoxy groups. Based on these results, a series of N-Cbz-alpha-amino-glutarimidooxy carboxylates derivatives (3a-e) were synthesized in moderate yield using a known synthetic procedure. Their anticonvulsant activities were evaluated using the maximal electroshock seizure (MES) test, the pentylene tetrazole induced seizure (PTZ) test, and the strychinine (Str) threshold test with the ultimate aim of developing more active anticonvulsants. None of the compounds (3a-e) tested showed anticonvulsant activity in the MES and PTZ test. However, all the compounds tested exhibited significant anticonvulsant activity in the Str. test. The most active compound in the Str. test was the methyl ester of N-Cbz-alpha-amino-glutarimidooxy acetic acid 3a (ED50 = 42.9 mg/kg).

译文

先前对N-Cbz-α-氨基戊二酰亚胺的抗惊厥活性的研究表明,N-Cbz-α-氨基-N-烷氧基戊二酰亚胺的衍生物具有显着的抗惊厥活性。此外,它们的抗惊厥活性取决于N-烷氧基的存在。基于这些结果,使用已知的合成方法以中等收率合成了一系列N-Cbz-α-氨基-戊二酰氧基羧酸盐衍生物 (3a-e)。使用最大电击癫痫发作 (MES) 测试,戊烯四唑诱发的癫痫发作 (PTZ) 测试和士冬氨酸 (Str) 阈值测试评估了其抗惊厥活性,最终目的是开发更活跃的抗惊厥药。在MES和PTZ测试中,测试的化合物 (3a-e) 均未显示抗惊厥活性。但是,所有测试的化合物在Str中均显示出显着的抗惊厥活性。测试。在Str.测试中最具活性的化合物是N-Cbz-α-氨基-戊二酰基氧乙酸3a的甲酯 (ED50 = 42.9 mg/kg)。

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