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Wyświetlanie 1-2 z 2
Tytuł:
SYNTHESIS AND ANTICONVULSANT PROPERTIES OF SOME N-ARYL AND N-ARYLAMINOMETHYL DERIVATIVES OF 3-P-ISOPROPOXYPHENYLPYRROLIDINE-2,5-DIONE
Autorzy:
Kocharov, Sergey L.
Panosyan, Henry
Chmielewski, Jaroslaw
Gworek, Barbara
Łuszczki, Jarogniew J.
Powiązania:
https://bibliotekanauki.pl/articles/895346.pdf
Data publikacji:
2019-04-30
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
maximal electroshock-induced seizures
3-p-Isopropoxyphenylpyrrolidine-2
5-dione
N-aryl derivatives
N-arylaminomethyl derivatives
Opis:
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.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 2; 265-273
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synthesis and study of substituted amides of some 5-membered isocyclic and heterocyclic acids as potential anticonvulsants
Autorzy:
STRUPIŃSKA, MARZANNA
JAKUBOWICZ, BARTŁOMIEJ
ROSTAFIŃSKA-SUCHAR, GRAŻYNA
PIRIANOWICZ-CHABER, ELŻBIETA
KONAROWSKA, MAGDALENA
MAZUREK, ALEKSANDER P.
Powiązania:
https://bibliotekanauki.pl/articles/895607.pdf
Data publikacji:
2018-06-30
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
Maximal electroshock seizure test
anticonvulsant activity
substituted benzylamides of isocyclic acids
substituted benzylamides of heterocyclic acids
psychomotor seizure test
Opis:
A series of substituted amides of isocyclic and heterocyclic acids have been synthesized. All obtained compounds were evaluated qualitatively for their anticonvulsant activity in the maximal electroshock seizure test (MES test) and psychomotor seizure test (6 Hz test) in mice after intraperitoneal administration. The neurological toxicity was determined in the rotorod neurotoxicity test (Tox test). Two of these compounds appeared most promising: 3-oxo-1-cyklopentanecarboxylic acid 2-fluorobenzylamide (5), 1-cyclopentenecarboxylic acid 2-(trifluoromethyl)benzylamide (8) and were tested quantitatively in MES test in mice after oral administration (o.p.) and in 6 Hz test in mice after intraperitoneal administration(i.p.). Compound (5) showed MES ED50 =82.65 mg/kg and compound (8) showed 6 Hz ED50=84.13 mg/kg.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 3
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł
    Wyświetlanie 1-2 z 2

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