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KMID : 0043319960190030248
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Archives of Pharmacal Research
1996 Volume.19 No. 3 p.248 ~ p.250
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Synthesis and Anticonvulsant Evaluation of a Series of N-Cbz-α-aminoglutarimides
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Lee Jae-Won
Choi Jong-Won
Park Min-Soo
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Abstract
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In conclusion, a series of N-Cbz-.alpha.-amono-glutarimides (1a-f), combining common structures such as N-CO-C-N and cyclic imide in a single molecule, were prepared from the (R)- or (S)-N-Cbz-glutamic acid and evaluated for their anticonvulsant activities in MES and PTZ tests in order to develope new and broad spectrum anticonvulsant. In this study, N-Cbz-.alpha.-aminoglutarimides (1) except ac and af, showed significant anticonvulsant activity in both MES and PTZ tests enough to be recommended as promising new anticonvulsant drug candidates. Now we are continuing to investigate further anticonvulsant test (quantification)for these compounds and synthesize their analogues in order to develop more active anticonvulsant and define the structure activity relationship more precisely.
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KEYWORD
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Anticonvulsant, Glutarimide, Maximal electric shock(MES), Pentylenetetrazole induced seizure(PTZ)
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