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

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Pharmaceutical Chemistry Journal Aims and scope

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.

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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, 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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  1. G. V. Mokrov
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  2. T. A. Voronina
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  3. S. A. Litvinova
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  4. I. G. Kovalev
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  5. L. N. Nerobkova
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  6. A. D. Durnev
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  7. T. A. Gudasheva
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  8. S. B. Seredenin
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Correspondence to G. V. Mokrov.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 53, No. 3, pp. 3 – 9, March, 2019.

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Mokrov, G.V., Voronina, T.A., Litvinova, S.A. et al. Synthesis and Anticonvulsant Activity of 4-Amino-3-Nitro-1-Thiocoumarins and 4-Amino-3-Nitroquinolin-2-Ones. Pharm Chem J 53, 194–200 (2019). https://doi.org/10.1007/s11094-019-01978-1

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  • DOI: https://doi.org/10.1007/s11094-019-01978-1

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