Anticonvulsant activity of 1‐alkyl‐4‐substituted 3,5‐pyrazolidinediones

M. J. Kornet, J. H. Thorstenson, W. C. Lubawy

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18 Scopus citations

Abstract

Methods were developed for the synthesis of 1‐methyl‐4‐substituted 3,5‐pyrazolidinediones. These compounds are related to phensuximide and diphenylhydantoin and were prepared as potential anticonvulsant agents. The reaction between substituted malonic esters and methylhydrazine in the presence of sodium methoxide was employed to prepare a series of 1‐methyl‐4,4‐disubstituted 3,5‐pyrazolidinediones. 1‐Methyl‐4‐phenyl‐3,5‐pyrazolidinedione was prepared from diethyl phenylmalonate and methylhydrazine. 1,4‐Diethyl‐4‐phenyl‐3,5‐pyrazolidinedione was obtained by the alkylation of 4‐ethyl‐4‐phenyl‐3,5‐pyrazolidinedione with ethyl bromide in the presence of potassium tert‐butoxide as the base. All compounds are novel and were characterized by elemental analysis and IR and PMR spectrometry. All products were evaluated by maximal electroshock seizure and pentylenetetrazol seizure threshold tests.

Original languageEnglish
Pages (from-to)1090-1093
Number of pages4
JournalJournal of Pharmaceutical Sciences
Volume63
Issue number7
DOIs
StatePublished - Jul 1974

Keywords

  • 1‐Methyl‐4,4‐disubstituted 3,5‐pyrazolidinediones—synthesis, evaluation of anticonvulsant activity
  • 3,5‐Pyrazolidinediones, 1‐methyl‐4,4‐disubstituted—synthesis, evaluation of anticonvulsant activity
  • Anticonvulsant activity—synthesis and evaluation of 1‐methyl‐4‐substituted 3,5‐pyrazolidinediones

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