Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 31, Issue 6, Pages 1576-1582Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2016.1158172
Keywords
Anticonvulsant drugs; epilepsy; PTZ model; rotarod test; thiazoles
Funding
- Nicolaus Copernicus University [786/2014]
- National Science Centre [DEC-2012/05/B/NZ7/02705]
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Synthesis, characterization and investigation of in vivo anticonvulsant activities of 13 novel cyclopentanecarbaldehyde-based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using H-1 and C-13 NMR, FAB(+)-MS, HRMS and elemental analyses. The results of anticonvulsant screening reveal that seven intraperitoneally administered compounds: 3a, 3b, 3d, 3e, 3f, 3k and 3m containing F-, Cl-, Br-, CF3-, CH3- and adamantyl substituents demonstrated significant anticonvulsant activity in the pentylenetetrazole model with median effective doses (ED50) <= 20 mg/kg, respectively, which was approximately seven-fold lower than that reported for the reference drug, ethosuximide. Noteworthy, none of these compounds impaired animals' motor skills in the rotarod test.
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