Development of 1, 3 Benzothiazol-2-yl Hydrazine Derivatives Containing Semicarbazone and Thioamide Pharmacophore as Anticonvulsants
Newer N-(6-substitutedbenzo[d]thiazol-2-yl)-2-((substitutedcarbamothioyl)hydrazinecarboxamides were synthesized
having semicarbazone and thioamide as two hydrogen bonding domains attached between proximal and distal
aryl rings with a view to explore prospective anticonvulsant candidates. For preliminary screening of synthesized compounds,
two convulsant tests i.e. Maximal electroshock (MES) and subcutaneous Pentylenetetrazole (scPTZ) tests were
performed. Rotarod test was performed to determine any possible neurotoxicity in the synthesized compounds. The result
of anticonvulsant screening established the significant ability of compounds, 3i, 3j and 3m, to suppress the convulsions
generated by electrical seizures and scPTZ induced seizures as compared to standard drugs phenytoin (PHY) and carbamazepine
(CBZ). Molecular properties and Pharmacokinetic parameters of the titled compounds were also determined using
Lipinski’s rule of five. The promising results encourage future investigation on the rational modification of this nucleus
for development of better compounds.
Keywords: Anticonvulsant, benzothiazole, semicarbazone, thioamide, pharmacokinetic, neurotoxicity.
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