Archives of Pharmacal Research
- 제21권6호
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- Pages.759-763
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- 1998
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- 0253-6269(pISSN)
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- 1976-3786(eISSN)
The Effect of N-Alkyloxycarbonyl Group on the Anticonvulsant Activities of N-Alkyloxycarbonyl-alpha-amino-N-methylsuccinimides
- Jung, Kyung-Im (College of Pharmacy, Kyungsung University) ;
- Son, Ki-Chun (College of Pharmacy, Kyungsung University) ;
- Kim, Min-Jeong (College of Pharmacy, Kyungsung University) ;
- Lee, Jae-Won (Koshin Medical Center) ;
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Choi, Jong-Won
(College of Pharmacy, Kyungsung University) ;
- Lee, Eung-Seok (Yeungnam University) ;
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Park, Min-Soo
(College of Pharmacy, Kyungsung University)
- 발행 : 1998.12.01
초록
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