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The Effect of N-Substituted Alkyl Groups on Anticonvulsant Activities of N-Cbz-$alpha$-amino-N-alkylglutarimides
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  • The Effect of N-Substituted Alkyl Groups on Anticonvulsant Activities of N-Cbz-$alpha$-amino-N-alkylglutarimides
  • The Effect of N-Substituted Alkyl Groups on Anticonvulsant Activities of N-Cbz-$alpha$-amino-N-alkylglutarimides
저자명
Lee. Jae-Won,Son. Ki-Chun,Jung. Gyung-Im,Kim. Min-Jeong,Choi. Jong-Won,Lee. Eung-Seok,Park. Min-Soo
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
1999년|22권 5호|pp.491-495 (5 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

In order to examine the effects of N-substituted alkyl group on the anticonvulsant activities of N-Cbz-$alpha$-aminoglutarimides as novel anticonvulsants with broad spectrum, a series of (R) or (S) N-Cbz-$alpha$-amino-N-alkylglutarimides (1 and 2) were prepared from the corresponding (R) or (S) N-Cbz-glutamic acid and evaluated for the anticonvulsant activities in the maximal electroshock seizure (MES) test and pentylenetetrazol induced seizure(PTZ) test, including the neurotoxicity. The most potent compound in the MES test was (S) N-Cbz-$alpha$-amino-N-methylglutarimide($ED_{50}$=36.3 mg/kg, PI=1.7). This compound was also most potent in the PTZ test ($ED_{50}$=12.5 mg/kg, PI=5.0). The order of anticonvulsant activities against the MES test as evaluated form $ED_{50}$ values for (R) series was N-methyl > N-H > N-ethyl > N-allyl ; for the (S) series N-methyl > N-H > N-ethyl > N-alkyl > N-isobutyl compound. Against the PTZ tests, the order of anticonvulsant activities showed similar pattern ; for the (R) series, N-methyl > N-H > N-ethyl > N-allyl ; for the (S) series N-methyl > N-H > N-ethyl > N-allyl > N-isobutyl compound. From the above results, N-substituted alkyl groups were though to play an important role for the anticonvulsant activities of N-Cbz-$alpha$-amino-N-alkylgutarimides.