title: Design, synthesis and anticonvulsant activities of novel 1-(substituted/unsubstituted benzylidene)-4-(4-(6,8-dibromo-2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl) semicarbazide derivatives.
abstract: Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and 5k were found active in the preliminary screening in MES model and/or scPTZ model. Further all these five compounds were administered to rats, 5c and 5d showed better activity than Phenytoin in oral route. Among all the title compounds tested, the most active one was 5c that revealed protection in MES at a dose of 30 mg/kg (ip) after 0.5 and 4h. This molecule also provided protection in the scPTZ at a dose of 100mg/kg (0.5h) and 300 mg/kg (4h).
authors.affiliation: Medicinal Chemistry Research Laboratory, Bapatla College of Pharmacy, Jawaharlal Nehru Technological University, Hyderabad, Andhra Pradesh, India. sarachem1981@gmail.com
authors.forename: Govindaraj
authors.initials: G
authors.lastname: Saravanan
authors.forename: Veerachamy
authors.initials: V
authors.lastname: Alagarsamy
authors.forename: Chinnasamy Rajaram
authors.initials: CR
authors.lastname: Prakash
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000009:adverse effects / Q000138:chemical synthesis*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D020258:Neurotoxicity Syndromes / Q000209:etiology; D052999:Quinazolinones / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D012640:Seizures / Q000517:prevention & control; D012663:Semicarbazides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D052999:Quinazolinones; D012663:Semicarbazides