Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

被引：11

作者：

El Batran S.A. ^{[1
]}

Osman A.E.N. ^{[2
]}

Ismail M.M. ^{[3
]}

El Sayed A.M. ^{[3
]}

机构：

[1] Pharmacology Department, National Research Center, Dokki, Cairo

[2] Department of Organic Chemistry, Faculty of Pharmacy, Cairo University

[3] Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University Nasr City, Cairo

来源：

InflammoPharmacology | 2006年 / 14卷 / 1-2期

关键词：

Analgesic; Anticonvulsant; Carbamazepine; Novalgine; Phenobarbital sodium; Sedative;

D O I：

10.1007/s10787-006-1498-4

中图分类号：

学科分类号：

摘要：

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 1a-g or cycloalkylidenes 3a,b which underwent Michael 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. © Birkhäuser Verlag, Basel, 2006.

引用

页码：62 / 71

页数：9

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