title: Synthesis, anticonvulsant and neurotoxicity evaluation of some newer N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide analogs.
abstract: A series of 12, N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide analogs was designed and synthesized to meet the pharmacophore requirement essential for anticonvulsant activity. All the compounds were characterized by IR, (1)H NMR and mass spectral data followed by their anticonvulsant evaluation according to the Antiepileptic Drug Development Program (ADD) protocol. The present study has proved the hypothesis concerning the pharmacophore model with essential binding sites. N-(2-benzoylbenzofuran-3-yl)-3-(4-(2-fluorophenyl)piperazin-1-yl) propanamide, 6h was found to be the most active compound in both maximal electroshock seizure (MES) and subcutaneous metrazol (scMET) seizure test at 30 and100 mg/kg respectively at 0.5 and 4.0 h.
authors.forename: Mehnaz
authors.initials: M
authors.lastname: Kamal
authors.forename: Ashok K
authors.initials: AK
authors.lastname: Shakya
authors.forename: Mohamed Jawed
authors.initials: MJ
authors.lastname: Ahsan
authors.affiliation: Faculty of Pharmacy, Integral University, Dasauli, Kursi Road, Lucknow, Uttar Pradesh 226 026, India. mailtomehnaz@gmail.com.
authors.forename: Talha
authors.initials: T
authors.lastname: Jawaid
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D003292:Convulsants; D015195:Drug Design; D004597:Electroshock; D007202:Indicators and Reagents; D051379:Mice; D009422:Nervous System Diseases / Q000139:chemically induced; D010433:Pentylenetetrazole; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy
chemical_list: D000927:Anticonvulsants; D001572:Benzofurans; D003292:Convulsants; D007202:Indicators and Reagents; C000593864:N-(2-benzoylbenzofuran-3-yl)-3-(4-(2-fluorophenyl)piperazin-1-yl)propanamide; D010879:Piperazines; D010433:Pentylenetetrazole