N-Acyl-alpha-aminoglutarimide 계 화합물의 항경련 활성에 대한 N-Acyl 기의 영향

• 영문명: The effect of N-Acyl Groups on the Aniticonvulsant Activities of N-Acyl-alpha-amino-N-mehtyglutarimides
• 발행기관: 대한약학회
• 저자명: 손기천(Kichun Son) 최종원(Jongwon Choi) 신은화(Eunhwa Shin) 박민수(Minsoo Park)
• 간행물 정보: 『약학회지』제45권 제1호 (2001년), 7~15쪽, 전체 9쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2001.02.28

영문 초록

For the purpose of defining the effects of N-acyl groups on the anticonvulsant activities of N-acyl-alpha-glutarimides, various (R)- and (S)-N-acyl-alpha- aminoglutarimide were prepared from the corresponding N-Cbz-glutamic acid and were evaluated their anticonvulsant activies in the MES and PTZ test, including their neurotoxicities. Among the tested compounds, only (R) N-cinnamoyl-alpha-amino-N-meth- ylglutarimide showed anticonvulsant activity in the MES and PTZ test. And the other tested compounds was active in the only PTZ test. The order of anticonvulsant activities in the PTZ test was as followes ; for the (R) series, N-4-methoxycinnamoyl = cinnamoyl > N-4-nitrobenzoyl > N-benzoyl > N-phenylacetyl ; for the (S) series, N- 4- methoxycinnamoyl = N-3-nitrobenzoyl > N-4-nitrobenzoyl = N-cinnamoyl = N- phenylacetyl. From the above results, it was conceivable that the substituted N-acyl group had important effects on the anticonvulsant activites of these compounds. However steroisomeric deferences in the anticonvulsant activities were not exhibited clearly.

키워드

Anticonvulsant activities PTZ test MES test N-acyl-a-aminoglutarimides