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Synthesis and study of substituted amides of some 5-membered isocyclic and heterocyclic acids as potential anticonvulsants

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STRUPIŃSKA M., JAKUBOWICZ B., ROSTAFIŃSKA-SUCHAR G., PIRIANOWICZ-CHABER E., KONAROWSKA M., MAZUREK A. P.
Acta Poloniae Pharmaceutica - Drug Research
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2018
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vol. 75
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issue 3
EN
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.
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