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


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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.

作者简介

G. Mokrov

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

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Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315

T. Voronina

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315

S. Litvinova

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315

I. Kovalev

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315

L. Nerobkova

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315

A. Durnev

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315

T. Gudasheva

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315

S. Seredenin

V. V. Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences

Email: g.mokrov@gmail.com
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315


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