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

• Authors: MARZANNA STRUPIŃSKA , BARTŁOMIEJ JAKUBOWICZ , GRAŻYNA ROSTAFIŃSKA-SUCHAR , ELŻBIETA PIRIANOWICZ-CHABER , MAGDALENA KONAROWSKA , ALEKSANDER P. MAZUREK
• Languages of publication: EN

Abstracts

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.

Keywords

EN

Maximal electroshock seizure test; anticonvulsant activity; substituted benzylamides of isocyclic acids; substituted benzylamides of heterocyclic acids; psychomotor seizure test

• Journal: Acta Poloniae Pharmaceutica - Drug Research
• Year: 2018
• Volume: 75
• Issue: 3

Dates

published

2018-06-30

Contributors

author

MARZANNA STRUPIŃSKA

author

BARTŁOMIEJ JAKUBOWICZ

author

GRAŻYNA ROSTAFIŃSKA-SUCHAR

author

ELŻBIETA PIRIANOWICZ-CHABER

author

MAGDALENA KONAROWSKA

author

ALEKSANDER P. MAZUREK