Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity
- Authors: Zhmurenko L.A.1, Litvinova S.A.1, Mokrov G.V.1, Kovalev I.G.1, Voronina T.A.1, Nerobkova L.N.1, Gudasheva T.A.1
-
Affiliations:
- V. V. Zakusov Research Institute of Pharmacology
- Issue: Vol 53, No 5 (2019)
- Pages: 429-435
- Section: Article
- URL: https://journals.rcsi.science/0091-150X/article/view/245797
- DOI: https://doi.org/10.1007/s11094-019-02015-x
- ID: 245797
Cite item
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.
About the authors
L. A. Zhmurenko
V. V. Zakusov Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
S. A. Litvinova
V. V. Zakusov Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
G. V. Mokrov
V. V. Zakusov Research Institute of Pharmacology
Author for correspondence.
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
I. G. Kovalev
V. V. Zakusov Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
T. A. Voronina
V. V. Zakusov Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
L. N. Nerobkova
V. V. Zakusov Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
T. A. Gudasheva
V. V. Zakusov Research Institute of Pharmacology
Email: g.mokrov@gmail.com
Russian Federation, 8 Baltiiskaya St., Moscow, 125315