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Pharmaceutical Chemistry Journal

, Volume 53, Issue 5, pp 429–435 | Cite as

Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity

  • L. A. Zhmurenko
  • S. A. Litvinova
  • G. V. MokrovEmail author
  • I. G. Kovalev
  • T. A. Voronina
  • L. N. Nerobkova
  • T. A. Gudasheva
Article
  • 13 Downloads

New 4-phenylpyrrolidone derivatives were designed from racetam structures that combine nootropic and anticonvulsant activity. The proposed compounds were synthesized using 4-phenylpyrrolidone and aromatic amines. The anticonvulsant activity of the new compounds was studied. The structure–activity relationship was analyzed. The most active compound was the 2,6-dimethylanilide of (2-oxo-4-phenylpyrrolidin-1-yl)acetic acid at doses of 2.5 – 5.0 mg/kg, which surpassed the reference drug levetiracetam at doses of 2.5 – 600 mg/kg in all tests and possessed distinct nootropic activity that was comparable to that of the reference nootropic drug piracetam at a dose of 400 mg/kg.

Keywords

4-phenylpyrrolidones anticonvulsant activity nootropic activity maximal stimulation voltage corazole antagonism test 

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • L. A. Zhmurenko
    • 1
  • S. A. Litvinova
    • 1
  • G. V. Mokrov
    • 1
    Email author
  • I. G. Kovalev
    • 1
  • T. A. Voronina
    • 1
  • L. N. Nerobkova
    • 1
  • T. A. Gudasheva
    • 1
  1. 1.V. V. Zakusov Research Institute of PharmacologyMoscowRussia

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