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

G. V. Mokrov; T. A. Voronina; S. A. Litvinova; I. G. Kovalev; L. N. Nerobkova; A. D. Durnev; T. A. Gudasheva; S. B. Seredenin

doi:10.1007/s11094-019-01978-1

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

Autores: 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
Afiliações:
1. V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Edição: Volume 53, Nº 3 (2019)
Páginas: 194-200
Seção: Search for New Drugs
URL: https://journals.rcsi.science/0091-150X/article/view/245680
DOI: https://doi.org/10.1007/s11094-019-01978-1
ID: 245680

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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.