YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

The effect of N-Acyl Groups on the Anticonvulsant Activities of N-Acyl -$\alpha$- amino-N-methylglutarimides

N-Acyl-$\alpha$-aminoglutarimide계 화합물의 항경련 활성에 대한 N-Acyl기의 영향

  • Published : 2001.02.01
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Abstract

For the purpose of defining the effects of N-acyl groups on the anticonvulsant activities of N-acyl-$\alpha$-amino-glutarimides, various (R)- and (S)-N-acyl-$\alpha$-aminoglutarimide were prepared from the corresponding N-Cbz-glutamic acid and were evaluated their anticonvulsant activities in the MES and PTZ test, including their neurotoxicities. Among the tested compounds, only (R) N-cinnamoyl-$\alpha$-amino-N-methylglutarimide 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 activities of these compounds. However stereoisomeric deferences in the anticonvulsant activities were not exhibited clearly.

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References

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