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

Abstract

A series of ( R)- and (S)-N- Cbz-α-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-α-amino- N-methyl glutarimide( 1d) and the ED 50 value in the MES test was 36.1 mg/kg and the ED 50 value in the PTZ test was 12.5 mg/kg. In the rotorod test for neurotoxicity, the TD 50 value was 62.5 mg/kg.