N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective

Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective

 

 

 

 

 

 

A series of N-(substituted benzothiazol-2-yl)amide derivatives 2a–h and 4a–h were synthesized by the EDC coupling reactions of substituted-benzothiazol-2-amine with 4-oxo-4-phenylbutanoic acid/2-benzoyl benzoic acid and evaluated for their anticonvulsant and neuroprotective effect.


 N-(6-methoxybenzothiazol-2-yl)-4-oxo-4-phenylbutanamide (2f) emerged as the most effective anticonvulsant with median doses of 40.96 mg/kg (MES ED₅₀), 85.16 mg/kg (scPTZ ED₅₀) and 347.6 mg/kg (TD₅₀).


Furthermore, compound 2f displayed promising neuroprotective effect by lowering the levels of MDA and LDH; therefore, it represents a potential lead in search for safer and effective anticonvulsants having neuroprotective effects.