Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities
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New 2,6-piperidinediones 2a–g and 4a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides la–g or cycloalkylidenes 3a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5a–m.
Some new selected compounds 2a–c,f, 4a–d & 5e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2f.
Keywords.Carbamazepine Phenobarbital sodium Novalgine Anticonvulsant Sedative Analgesic
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