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- Title
Synthesis and Study of Psychotropic Activity of 1-Substituted 4-Amino-5-oxoprolines.
- Authors
Vigorov, A. Yu.; Krasnov, V. P.; Nizova, I. A.; Sadretdinova, L. Sh.; Levit, G. L.; Matveeva, T. V.; Slepukhin, P. A.; Bakulin, D. A.; Kovalyov, N. S.; Tyurenkov, I. N.; Charushin, V. N.
- Abstract
1-Substituted (2S,4S)-4-amino-5-oxoprolines have been obtained by nucleophilic substitution of bromine in dimethyl (2S,4RS)-4-bromo-N-phthaloylglutamate followed by isolation of the predominant (2S,4S)-diastereomer and removal of protecting groups. The psychotropic activity of the obtained compounds has been studied after a single administration in experimental animals. 4-Amino-1-(4-bromophenyl)-5-oxoproline and especially 4-amino-1-(4-aminophenyl)-5-oxoproline showed pronounced anxiolytic activity in the Elevated plus maze test. (2S,4S)-4-Amino-5-oxoprolines containing 4-methylphenyl, 4-bromophenyl, 4‑aminophenyl, and 2,3-dimethyl-5-oxo-1-phenyl-3-pyrazolin-4-yl substituents at the 1-position exhibited nootropic activity: they improved the formation and retention of the memory trace in the Passive avoidance test and the Active avoidance test (Extrapolation escape test).
- Subjects
TROPANES; MAZE tests; LABORATORY animals; BROMINE; AROMATIC amines; EXTRAPOLATION
- Publication
Doklady Chemistry, 2020, Vol 494, Issue 1, p131
- ISSN
0012-5008
- Publication type
Article
- DOI
10.1134/S0012500820090049