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The Effect of N-Alkyloxycarbonyl Group on the Anticonvulsant Activities of N-Alkyloxycarbonyl-alpha-amino-N-methylsuccinimides
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  • The Effect of N-Alkyloxycarbonyl Group on the Anticonvulsant Activities of N-Alkyloxycarbonyl-alpha-amino-N-methylsuccinimides
  • The Effect of N-Alkyloxycarbonyl Group on the Anticonvulsant Activities of N-Alkyloxycarbonyl-alpha-amino-N-methylsuccinimides
저자명
Jung. Kyung-Im,Son. Ki-Chun,Kim. Min-Jeong,Lee. Jae-Won,Choi. Jong-Won,Lee. Eung-Seok,Park. Min-Soo
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
1998년|21권 6호|pp.759-763 (5 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

In connection with the development of new anticonvulsant agents with a broad spectrum, we found that N-Cbz-alpha-amino-alkylsuccinimides showed significant anticonvulsant activities, and the pharmacological activities of these compounds were dependent on their stereochemistry and N-substituted alkyl group. These results prompted us to define the effects of other functional group on the anticonvulsant activities of these compounds. Therefore a series of N-alkoxycarbonyl-alpha-amino-N-methylsuccinimide were prepared from N-Cbz-aspartic acid and were evaluated with their anticonvulsant activities againt the MES and PTZ tests, in order to define the effect of N-substituted alkoxy carbonyl group with the anticonvulsant activities. From these studies, it was found that all the tested N-alkoxycarbonyl-alpha-amino-N-methylsuccinimides exhibited significant anticonvulsant activities in the PTZ test and were not active in the MES test. The most active compound in the PTZ test was (S) N-ethoxycarbonyl-alpha-amino-N-methyl-succinimide. We found that the pharmacological activities in the PTZ test were dependent on their N-alkoxycarbonyl groups. They follow as such: The order of anticonvulsant activities for (R) series as evaluated by $ED_{50}$ was N-phenoxycarbonyl=N-4-nitrobenzyloxycarbonyl > N-ethoxycarbonyl > N-allyloxycarbonyl > N-tert. butoxycarbonyl compound: For the (S) series N-ethoxycarbonyl > N-phenoxycarbonyl > N-allyloxycarbonyl compound. From the above results, it was conceivable that N-substituted alkoxycarbonyl group had certain effects on the anticonvulsant activities of N-alkoxycarbonyl-${alpha}$-amino-N-methylsuccinimides.