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

• Authors: Sergey L. Kocharov , Henry Panosyan , Jaroslaw Chmielewski , Barbara Gworek , Jarogniew J. Łuszczki
• Languages of publication: EN

Abstracts

EN

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.

Keywords

EN

maximal electroshock-induced seizures; 3-p-Isopropoxyphenylpyrrolidine-2; 5-dione; N-aryl derivatives; N-arylaminomethyl derivatives

• Journal: Acta Poloniae Pharmaceutica - Drug Research
• Year: 2019
• Volume: 76
• Issue: 2
• Pages: 265-273

Dates

published

2019-04-30

Contributors

author

Sergey L. Kocharov

author

Henry Panosyan

author

Jaroslaw Chmielewski

author

Barbara Gworek

author

Jarogniew J. Łuszczki

Identifiers

DOI

10.32383/appdr/97323