Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 67, Issue -, Pages 1-13Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.06.026
Keywords
Benzothiazole; 4-Oxoquinazoline-3(4H)-carbothioamide; Anticonvulsant activity; Neuroprotection; AMPA induced seizure
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Funding
- Central Scientific Industrial Research (CSIR) New Delhi, India
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Novel N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives were synthesized and evaluation of their anticonvulsant effects was done using various models of experimental epilepsy. Initial anticonvulsant activities of the compounds were investigated using intraperitoneal (i.p.) maximal electroshock shock (MES), subcutaneous pentylenetetrazole (scPTZ) seizure models in mice. The quantitative assessment after oral administration in rats showed that the most active was 2-methy1-4-oxo-N-(6-(trifluoromethoxy)benzo[d]thiazol-2-ylcarbamoyl)quinazoline-3(4H)-carbothioamide (SA 24) with ED50 values of 82.5 mu mol/kg (MES) and 510.5 mu mol/kg (scPTZ). This molecule was more potent than phenytoin and ethosuximide which were used as reference antiepileptic drugs. To explain the possible mechanism for anticonvulsant action, some of the selected active compounds were subjected to GABA (gamma-amino butyric acid) assay and AMPA ((S)-2-amino-3-(3-hydroxyl-5-methyl-4-isoxazolyl) propionic acid) induced seizure test. (C) 2013 Elsevier Masson SAS. All rights reserved.
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