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InflammoPharmacology

, Volume 14, Issue 1–2, pp 62–71 | Cite as

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

  • S. A. El Batran
  • A. E. N. Osman
  • M. M. Ismail
  • A. M. El Sayed
Short Communication

Abstract.

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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Copyright information

© Birkhäuser Verlag, Basel 2006

Authors and Affiliations

  • S. A. El Batran
    • 1
  • A. E. N. Osman
    • 2
  • M. M. Ismail
    • 3
  • A. M. El Sayed
    • 3
  1. 1.Pharmacology DepartmentNational Research CenterCairoEgypt
  2. 2.Department of Organic Chemistry, Faculty of PharmacyCairo UniversityCairoEgypt
  3. 3.Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls)Al-Azhar University Nasr CityCairoEgypt

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