title: Design and synthesis of anticonvulsants from a combined phthalimide-GABA-anilide and hydrazone pharmacophore.
abstract: Two series of pharmacophoric hybrids of phthalimide-GABA-anilides/hydrazones were designed and synthesized and evaluated for their anticonvulsant and neurotoxic properties. The structures of the synthesized compounds were confirmed by the use of their spectral data besides elemental analysis. Initial anticonvulsant screening was performed using intraperitoneal (i.p.) maximal electroshock-induced seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcutaneous strychnine (scSTY), and intraperitoneal picrotoxin (ipPIC)-induced seizure threshold tests. All of the compounds were ineffective in the MES test. Most of the compounds were found to be effective in the scSTY and ipPIC models and very few compounds showed protection in the scPTZ model.
authors.affiliation: Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Vidya Vihar, Pilani, Rajasthan 333031, India.
authors.forename: Jegadeesan Vaigunda
authors.initials: JV
authors.lastname: Ragavendran
authors.forename: Dharmarajan
authors.initials: D
authors.lastname: Sriram
authors.forename: Sravan Kumar
authors.initials: SK
authors.lastname: Patel
authors.forename: Ingala Vikram
authors.initials: IV
authors.lastname: Reddy
authors.forename: Narayanan
authors.initials: N
authors.lastname: Bharathwajan
authors.forename: James
authors.initials: J
authors.lastname: Stables
authors.forename: Perumal
authors.initials: P
authors.lastname: Yogeeswari
mesh_terms: D000813:Anilides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D004195:Disease Models, Animal; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology; D045442:Rotarod Performance Test; D012640:Seizures / Q000188:drug therapy / Q000209:etiology / Q000517:prevention & control; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000813:Anilides; D000927:Anticonvulsants; D006835:Hydrazones; D010797:Phthalimides; D005680:gamma-Aminobutyric Acid