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

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

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-ami...

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Veröffentlicht in:Pharmaceutical chemistry journal 2019-06, Vol.53 (3), p.194-200
Hauptverfasser: Mokrov, G. V., Voronina, T. A., Litvinova, S. A., Kovalev, I. G., Nerobkova, L. N., Durnev, A. D., Gudasheva, T. A., Seredenin, S. B.
Format: Artikel
Sprache:eng
Schlagworte:
Anticonvulsants
Epilepsy
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Search for New Drugs
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Zusammenfassung: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.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-019-01978-1