Synthesis and Anticonvulsant Activity of 4-Amino-3-Nitro-1-Thiocoumarins and 4-Amino-3-Nitroquinolin-2-Ones
- 3 Downloads
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.
Keywordsthiocoumarins quinnolin-2-ones anticonvulsant activity maximal electroshock test corazole antagonism test
- 1.G. V. Mokrov, V. L. Savel’ev, T. A. Voronina, et al., Khim-farm. Zh., 53(2), 25 – 31 (2019).Google Scholar
- 3.V. L. Savel’ev, T. G. Afanas’eva, and V. A. Zagorevskii, Khim. Geterotsikl. Soedin., No. 1, 43 – 47 (1978).Google Scholar
- 9.T. A. Voronina and L. N. Nerobkova, Methodical Instructions for Studying Anticonvulsant Activity of Drugs “Handbook for Preclinical Drug Trials” [in Russian], Part 1, FGBU NTsEMSP, Grif i K, Moscow (2012), pp. 235 – 250.Google Scholar