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Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity.

Authors :
Zhmurenko, L. A.
Litvinova, S. A.
Mokrov, G. V.
Kovalev, I. G.
Voronina, T. A.
Nerobkova, L. N.
Gudasheva, T. A.
Source :
Pharmaceutical Chemistry Journal; Aug2019, Vol. 53 Issue 5, p429-435, 7p
Publication Year :
2019

Abstract

New 4-phenylpyrrolidone derivatives were designed from racetam structures that combine nootropic and anticonvulsant activity. The proposed compounds were synthesized using 4-phenylpyrrolidone and aromatic amines. The anticonvulsant activity of the new compounds was studied. The structure–activity relationship was analyzed. The most active compound was the 2,6-dimethylanilide of (2-oxo-4-phenylpyrrolidin-1-yl)acetic acid at doses of 2.5 – 5.0 mg/kg, which surpassed the reference drug levetiracetam at doses of 2.5 – 600 mg/kg in all tests and possessed distinct nootropic activity that was comparable to that of the reference nootropic drug piracetam at a dose of 400 mg/kg. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
0091150X
Volume :
53
Issue :
5
Database :
Complementary Index
Journal :
Pharmaceutical Chemistry Journal
Publication Type :
Academic Journal
Accession number :
172438963
Full Text :
https://doi.org/10.1007/s11094-019-02015-x