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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.

Acta Poloniae Pharmaceutica - Drug Research

2019

vol. 76

issue 2

265-273

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.

Pharmaceuticals in aquatic environment. Fate and behaviour, ecotoxicology and risk assessment – A review

86%

Gworek B., Kijeńska M., Zaborowska M., Wrzosek J., Tokarz L., Chmielewski J.

Acta Poloniae Pharmaceutica - Drug Research

2019

vol. 76

issue 3

397-407

Pharmaceuticals are long-lasting, biologically active substances that, when discharged into the natural environment, affect ecosystem stability. The presence of increasing amounts of pharmaceuticals and their transformation products in the environment has been a subject of growing interest. Many of the commonly used pharmaceuticals, especially analgesics and antibiotics, are used in quantities similar to those of agricultural chemicals, but are not required to undergo the same level of environmental risk assessment. The fate and behavior of medicines in the environment require further research. Human and veterinary pharmaceuticals and their metabolites are distributed in the environment in various ways. The incidence of medicines and their transformation products has been so far recorded in surface and ground waters, drinking water, bottom sediments, soils, wastewater and sewage sludge, as well as in animal organisms. The article presents issues related to the fate and behavior of pharmaceuticals both in the environment and in the processes of wastewater treatment, ecotoxicology and risk assessment.

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2 Acta Poloniae Pharmaceutica - Drug Research

2 2019

2 Chmielewski J.

2 Gworek B.

1 Kijeńska M.

1 Kocharov S. L.

1 Panosyan H.

1 Tokarz L.

1 Wrzosek J.

1 Zaborowska M.

1 Łuszczki J. J.

Search results

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

Pharmaceuticals in aquatic environment. Fate and behaviour, ecotoxicology and risk assessment – A review