Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
作者： Sachin Malik , Radhe Shyam Bahare , Suroor Ahmad Khan
DOI: 10.1016/J.EJMECH.2013.06.026
关键词:
摘要: 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 experimental epilepsy. Initial activities the compounds investigated intraperitoneal (i.p.) maximal electroshock shock (MES), subcutaneous pentylenetetrazole (scPTZ) seizure in mice. The quantitative assessment after oral administration rats showed that most active 2-methyl-4-oxo-N-(6-(trifluoromethoxy)benzo[d]thiazol-2-ylcarbamoyl)quinazoline-3(4H)-carbothioamide (SA 24) with ED50 values 82.5 μmol/kg (MES) 510.5 μmol/kg (scPTZ). This molecule more potent than phenytoin ethosuximide which used as reference antiepileptic drugs. To explain possible mechanism for action, some selected subjected to GABA (γ-amino butyric acid) assay AMPA ((S)-2-amino-3-(3-hydroxyl-5-methyl-4-isoxazolyl) propionic induced test.
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