title: Phenytoin-based bivalent ligands: design, synthesis and anticonvulsant activity.
abstract: Synthesis, characterization and anticonvulsant properties of new bivalent ligands derived from phenytoin were described. Initial anticonvulsant screening was performed using maximal electroshock (MES) and pentylenetetrazole (PTZ) screens in mice. The neurotoxicity for compounds that showed significant anticonvulsant activity was determined applying the rotorod test. Most of the test compounds were found to be effective in at least one seizure model in a dose of 100 mg/kg. Compound 5e exhibited marked anticonvulsant activity in both MES and PTZ screens. The computer-aided prediction of biological activity was carried out.
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
authors.forename: Samir
authors.initials: S
authors.lastname: Botros
authors.forename: Nadia A
authors.initials: NA
authors.lastname: Khalil
authors.forename: Bassem H
authors.initials: BH
authors.lastname: Naguib
authors.forename: Yara
authors.initials: Y
authors.lastname: El-Dash
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004597:Electroshock / Q000009:adverse effects / Q000379:methods; D005260:Female; D008024:Ligands; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000633:toxicity; D010672:Phenytoin / Q000138:chemical synthesis* / Q000627:therapeutic use*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control*; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D008024:Ligands; D010672:Phenytoin; D010433:Pentylenetetrazole