Studies on the Synthesis and Central Nervous Depressant Activities of Piperine Derivatives(IV) -Piperine Derivatives with Substituents in Piperidine Residue-

피페린유도체의 합성 및 중추 억제작용에 관한 연구(IV) -피페리딘에 치환기를 도입한 피페린유도체-

In order to search a more active and safer compound, piperine derivatives with substituents in piperidine residue were synthesized and evaluated on CNS depressant activity. N-Piperoyl-2-methylpiperidine (I) and N-piperoyl-3-methylpiperidine (II) were potent in strychnine-induced convulsion. Compound I and N-piperoyl-3-hydroxypiperidine (IX) exhibited a potent inhibitory effect againt pentetrazoleinduced convulsion and a significant prolongation effect of hexobarbital-induced sleeping time. The hydroxy derivatives were more toxic than the methyl derivatives.