Synthesis and Anticonvulsive Activity of 3- and 4-Benzoylpyridine Oxime Derivatives

  • L. A. Zhmurenko
  • T. A. Voronina
  • S. A. Litvinova
  • L. N. Nerobkova
  • I. O. Gaidukov
  • G. V. Mokrov
  • T. A. Gudasheva
Article
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We present here the synthesis of 3- and 4-benzoylpyridine oxime derivatives with potential anticonvulsant action. The most active compound in the maximum electric shock test was 4-benzoylpyridine O-2-morpholinoethyloxime oxalate (1a), i.p. doses of 60 – 150 mg/kg of which increased the survival of mice to 100%. The best effect in the corasol antagonism test was obtained with 4-benzoylpyridine O-(isonicotinoyl)oxime (2c), i.p. doses of 12.5 mg/kg of which increased the survival of mice to 67% and the latent period of onset of generalized tonic-clonic convulsions to 52 sec. Compound 1a had low toxicity (the i.p. LD50 in mice was 316 mg/kg) and a therapeutic index of 21.

Keywords

3- and 4-benzoylpyridine oximes anticonvulsant activity maximum electric shock test corasol antagonism test 

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  • L. A. Zhmurenko
    • 1
  • T. A. Voronina
    • 1
  • S. A. Litvinova
    • 1
  • L. N. Nerobkova
    • 1
  • I. O. Gaidukov
    • 1
  • G. V. Mokrov
    • 1
  • T. A. Gudasheva
    • 1
  1. 1.V. V. Zakusov Science Research Institute of PharmacologyMoscowRussia

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