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.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 53, No. 5, pp. 20 – 27, May, 2019.
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Zhmurenko, L.A., Litvinova, S.A., Mokrov, G.V. et al. Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity. Pharm Chem J 53, 429–435 (2019). https://doi.org/10.1007/s11094-019-02015-x
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DOI: https://doi.org/10.1007/s11094-019-02015-x