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Synthesis and Anticonvulsant Activity of 4-Amino-3-Nitro-1-Thiocoumarins and 4-Amino-3-Nitroquinolin-2-Ones

  • G. V. MokrovEmail author
  • T. A. Voronina
  • S. A. Litvinova
  • I. G. Kovalev
  • L. N. Nerobkova
  • A. D. Durnev
  • T. A. Gudasheva
  • S. B. Seredenin
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Novel thiocoumarins and quinolin-2-ones were synthesized and screened for anticonvulsant activity. The structure–activity relationship of a series of synthesized compounds and previously prepared coumarin derivatives was analyzed. The methyl ester of N-(3-nitro-2-oxo-1,2-dihydroquinolin-4-yl)-4-aminobutyric acid (3a) at a dose of 12.5 mg/kg (i.p.) had the greatest anticonvulsant activity in mouse tests.

Keywords

thiocoumarins quinnolin-2-ones anticonvulsant activity maximal electroshock test corazole antagonism test 

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Copyright information

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

Authors and Affiliations

  • G. V. Mokrov
    • 1
    Email author
  • T. A. Voronina
    • 1
  • S. A. Litvinova
    • 1
  • I. G. Kovalev
    • 1
  • L. N. Nerobkova
    • 1
  • A. D. Durnev
    • 1
  • T. A. Gudasheva
    • 1
  • S. B. Seredenin
    • 1
  1. 1.V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical SciencesMoscowRussia

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