title: Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi 110062, India.
authors.forename: Mohd Zaheen
authors.initials: MZ
authors.lastname: Hassan
authors.forename: Suroor A
authors.initials: SA
authors.lastname: Khan
authors.forename: Mohd
authors.initials: M
authors.lastname: Amir
mesh_terms: D020106:Acrylamide; D000577:Amides / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D052160:Benzothiazoles / Q000737:chemistry*; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005260:Female; D008297:Male; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D018696:Neuroprotective Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D010433:Pentylenetetrazole; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D013550:Swimming
chemical_list: D000577:Amides; D000927:Anticonvulsants; D052160:Benzothiazoles; D018696:Neuroprotective Agents; D020106:Acrylamide; C005465:benzothiazole; D010433:Pentylenetetrazole