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KMID : 0043320060290060459
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Archives of Pharmacal Research
2006 Volume.29 No. 6 p.459 ~ p.463
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Synthesis and Anticonvulsant Activities of N-Cbz-α-aminoglutarimidooxy Carboxylate
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Byun Ae-Sun
Choi Jong-Won
Moon Kyung-Ho
Lee Chung-Gyu
Park Min-Soo
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Abstract
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Previous studies on the anticonvulsant activity of N-Cbz-α-aminoglutarimides have shown that the derivatives of N-Cbz-α-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-α-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-α-amino-glutarimidooxy acetic acid 3a (ED50 = 42.9 mg/kg).
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KEYWORD
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Anticonvulsant, MES test, PTZ test, Strychnine threshold test, Glutarimide, Glutarimidooxy carboxylate
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