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Synthesis and Anticonvulsant Evaluations of N-Cbz-$alpha$-amino-N- alkoxyglutarimides
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  • Synthesis and Anticonvulsant Evaluations of N-Cbz-$alpha$-amino-N- alkoxyglutarimides
  • Synthesis and Anticonvulsant Evaluations of N-Cbz-$alpha$-amino-N- alkoxyglutarimides
저자명
Kim. Min-Jeong,Byun. Ae-Sun,Choi. Jong-Won,Moon. Kyung-Ho,Lee. Chung-Kyu,Park. Min-Soo
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2004년|27권 2호|pp.151-155 (5 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

In our previous studies for the development of new anticonvulsant of broad spectrum, we found that N-cbz-$alpha$-aminoglutarimides showed significant anticonvulsant activities of broad spectrum enough to be recommended for the new anticonvulsants and their anticonvulsant activities were dependent on their imide substituent groups. Based on these results, various N-cbz--$alpha$-amino-N-alkoxyglutarimides, where the imide N-H was substituted with the hydroxy and alkoxy group, were prepared and evaluated for their anticonvulsant activities using the Maximal electroshock seizure (MES) and Pentylenetetrazole induced seizure (PTZ) tests and also the rotorod test. A series of (R) or (S)-N-cbz--$alpha$-amino-N-alkoxyglutarimides could be prepared from the corresponding (R) or (S)-N-cbz-glutamic acid following the usual synthetic procedure. Among them, (R)-N-cbz--$alpha$-amino-N-hydroxyglutarimide ($ED_{50}$=86.25 mg/kg) was most active in the MES test. In the case of the PTZ test, (R)-N-cbz--$alpha$-amino-N-benzyloxyglutarimide ($ED_{50}$= 62.5 mg/kg) was most active. Among the tested compounds, 2a-c, 3a, and 3b showed anticonvulsant activities in the MES and PTZ test. All of the tested compounds, except 2f and 3f, showed significant anticonvulsant activities in the MES or PTZ test. In addition, the neurotoxicities of these compounds were comparable to other anticonvulsant drugs.