title: Anticonvulsant evaluation of some newer benzimidazole derivatives: design and synthesis.
abstract: A series of new 2-[(1-substituted phenylethylidine) hydrazine]-N-phenyl-1H-benzo[d]imidazole-1-carbothioamides (4a-n) were designed and synthesized to have the pharmacophoric elements essential for anticonvulsant activity. The key step in the synthesis of the title compounds involves the reaction of 2-mercaptobenzimidazole with hydrazine hydrate, substituted acetophenones and phenylisothiocyanate to get the compounds in good yields. All the newly synthesized compounds were screened by two most adopted models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). Interestingly, compounds 4e, 4f, 4g, 4h and 4j exhibited potent anticonvulsant results and in the neurotoxicity screening, most of the compounds were devoid of toxicity at the dose of 60 and 100 mg/kg.
authors.affiliation: Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, U.P. 281006, India.
authors.forename: Bhanupriya
authors.initials: B
authors.lastname: Bhrigu
authors.forename: Nadeem
authors.initials: N
authors.lastname: Siddiqui
authors.forename: Devender
authors.initials: D
authors.lastname: Pathak
authors.forename: M Shamsher
authors.initials: MS
authors.lastname: Alam
authors.forename: Ruhi
authors.initials: R
authors.lastname: Ali
authors.forename: Bishmillah
authors.initials: B
authors.lastname: Azad
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004558:Electric Stimulation; D005260:Female; D008297:Male; D015394:Molecular Structure; D010433:Pentylenetetrazole; D051381:Rats; D012640:Seizures / Q000209:etiology / Q000517:prevention & control*; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D001562:Benzimidazoles; C031000:benzimidazole; D010433:Pentylenetetrazole