Synthesis and anticonvulsant evaluation of a series of (R)- and (S)-N-Cbz-α-aminoglutarimide and succinimide

Bioorganic & Medicinal Chemistry Letters
1996.0

Abstract

A series of (R)- and (S)-N-Cbz-ct-aminoimides(1 and 2) were synthesized and were investigated their anticonvulsant activities in the MES and PTZ test, and determined the neurotoxicities. The most active compound among them was (S)-N-Cbz-c~-amino-N-methyl glutarimide(ld) and the ED50 value in the MES test was 36.1 mg/kg and the EDs0 value in the PTZ test was 12.5 mg/kg. In the rotorod test for neurotoxicity, the TDso value was 62.5 mg/kg.

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