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SYNTHESIS AND ANTICONVULSANT PROPERTIES OF SOME N-ARYL AND N-ARYLAMINOMETHYL DERIVATIVES OF 3-P-ISOPROPOXYPHENYLPYRROLIDINE-2,5-DIONE

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Kocharov S. L., Panosyan H., Chmielewski J., Gworek B., Łuszczki J. J.

Introduction: Anticonvulsant properties of newly synthesized compounds and potential antiepileptic drugs are usually assessed in screen tests in experimental animals. One of the most commonly used screen tests in mice is the maximal electroshock-induced seizure test that reflects tonic-clonic seizures in humans. Materials and Method: A series of 3-p-isopropoxyphenylpyrrolidine-2,5-dione derivatives, including N-aryl and N-arylaminomethyl analogs, were characterized for their anticonvulsant properties in the maximal electroshock-induced seizure test in mice. Electroconvulsions (tonic-clonic seizures) were evoked in adult Albino Swiss mice by a current (sine-wave, 25mA, 50Hz, 500V, 0.2s stimulus duration) delivered via auricular electrodes. Results: N-aryl derivatives did not show any anticonvulsant activity, whereas some representatives of N-arylaminomethyl derivatives, i.e. N-Mannich bases, exhibited a distinct protective action against maximal electroshock-induced (MES) convulsions in mice. Conclusions: Several N-arylaminomethyl derivatives of 3-p-isopropoxyphenylpyrrolidine-2,5-dione may become in future new antiepileptic drugs, or they could serve as valuable supporting materials for obtaining new derivatives with stronger anticonvulsant activities than their maternal compounds.

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1 Acta Poloniae Pharmaceutica - Drug Research

1 2019

1 Chmielewski J.

1 Gworek B.

1 Kocharov S. L.

1 Panosyan H.

1 Łuszczki J. J.

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SYNTHESIS AND ANTICONVULSANT PROPERTIES OF SOME N-ARYL AND N-ARYLAMINOMETHYL DERIVATIVES OF 3-P-ISOPROPOXYPHENYLPYRROLIDINE-2,5-DIONE