A newer series of 1-(4-substitutedphenyl)-3-(4-((2,4-dioxothiazolidin-5-lidene)methyl)phenyl
sulfonyl)urea/thiourea (4a-l) were synthesized for their anticonvulsant activity. The activity is attributed
to its potential to restrain astrocytic Na+, 2HCl, and K+ co-transport similar to torasemide which
has sulfonylurea in its structure. Torasemide having the similar action as the furosemide that obstructs
kainic acid-induced electrical discharges observed from cortex and it has neuroprotective agents, for
instance antagonizing the N-methyl-D-aspartate (NMDA) and non-NMDA receptors for evaluating
antiepileptic activity. The structures of new derivatives were established by elemental analysis and
spectroscopic techniques viz. FTIR, 1H NMR and LC-MS. The all twelve derivatives were assessed for anticonvulsant activity
at three different doses at 30, 100 and 300 mg/kg body weight into maximal electroshock (MES) and subcutaneous
pentylenetetrazole (sports) models. Compounds 4c and 4e were formed to be most active among all the derivatives for
both the models of anticonvulsant activity. Beside these compounds 4g, 4i and 4k also possessed the prominent anticonvulsant
activity devoid of any neurotoxicity. The sulfonylurea and sulfonylthiourea both were proved to be effective anticonvulsant
pharmacophore. Other structure activity relationships were established by considering the aspect of substitution
in the lead.
Keywords: Anticonvulsant, Sulfonylthiourea, Neurotoxicity, Thiourea.
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