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Synthesis and Anticonvulsant Activity of N-Substituted 4-Amino-3-Nitrocoumarins

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Pharmaceutical Chemistry Journal Aims and scope

The synthesis and anticonvulsant activity of new coumarin derivatives are reported. N-(3-Nitrocoumarin-4-yl)-4-aminobutyric acid (1a) at doses of 60 and 80 mg/kg (in the MES test) and methyl N-(3,6-dinitrocoumarin-4-yl)-4-aminobutyrate (1e) at doses of 20 and 40 mg/kg (in the corazole antagonism test) possessed the greatest anticonvulsant activity of the synthesized compounds. The results indicated that the coumarin derivatives were promising for further development as potential anticonvulsant agents.

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Acknowledgments

A. O. Dmitrienko thanks the Russian Science Foundation (Project No. 16-13-10404) for financial support for the structural studies of 1a.

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Authors and Affiliations

  1. V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences, 8 Baltiiskaya St., Moscow, 125315, Russia

    G. V. Mokrov, V. L. Savel’ev, T. A. Voronina, S. A. Litvinova, I. G. Kovalev, L. N. Nerobkova, T. A. Gudasheva & S. B. Seredenin

  2. A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, 28 Vavilova St., Moscow, 119991, Russia

    A. O. Dmitrienko

Authors
  1. G. V. Mokrov
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  2. V. L. Savel’ev
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  3. T. A. Voronina
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  4. S. A. Litvinova
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  5. I. G. Kovalev
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  6. L. N. Nerobkova
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  7. A. O. Dmitrienko
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  8. T. A. Gudasheva
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  9. S. B. Seredenin
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Corresponding author

Correspondence to G. V. Mokrov.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 53, No. 2, pp. 25 – 31, February, 2019.

V. L. Savel’ev is deceased.

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Mokrov, G.V., Savel’ev, V.L., Voronina, T.A. et al. Synthesis and Anticonvulsant Activity of N-Substituted 4-Amino-3-Nitrocoumarins. Pharm Chem J 53, 118–124 (2019). https://doi.org/10.1007/s11094-019-01964-7

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  • DOI: https://doi.org/10.1007/s11094-019-01964-7

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