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  • Design, synthesis and evaluation of 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.

European journal of medicinal chemistry (2012-11-06)
Mohd Zaheen Hassan, Suroor A Khan, Mohd Amir
ABSTRACT

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 ED(50)), 85.16 mg/kg (scPTZ ED(50)) and 347.6 mg/kg (TD(50)). 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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Benzothiazole, 96%
SKU
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Sigma-Aldrich
Benzothiazole, ≥96%, FG
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