Email this article Synthesis and Anticonvulsant Activity of 4-Amino-3-Nitro-1-Thiocoumarins and 4-Amino-3-Nitroquinolin-2-Ones
- Authors: Mokrov G.V.1, Voronina T.A.1, Litvinova S.A.1, Kovalev I.G.1, Nerobkova L.N.1, Durnev A.D.1, Gudasheva T.A.1, Seredenin S.B.1
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Affiliations:
- V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
- Issue: Vol 53, No 3 (2019)
- Pages: 194-200
- Section: Search for New Drugs
- URL: https://ogarev-online.ru/0091-150X/article/view/245680
- DOI: https://doi.org/10.1007/s11094-019-01978-1
- ID: 245680
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Abstract
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.
About the authors
G. V. Mokrov
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Author for correspondence.
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
T. A. Voronina
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
S. A. Litvinova
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
I. G. Kovalev
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
L. N. Nerobkova
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
A. D. Durnev
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
T. A. Gudasheva
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
S. B. Seredenin
V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
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