title: Synthesis and primary anticonvulsant activity evaluation of 6-alkyoxyl-tetrazolo [5,1-a]phthalazine derivatives.
abstract: A new series of 6-alkyoxyl-tetrazolo[5,1-a] phthalazine derivatives (4 a-4 o) were synthesized as potential anticonvulsant agents. Anticonvulsant activity was evaluated by the maximal electroshock (MES) test. Neurotoxicity was evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 6-(4-chlorophenyoxyl)-tetrazolo[5,1-a]phthalazine (4 m) was the most potent agent, with a median effective dose (ED50) of 6.8 mg/kg and a median neurotoxic dose (TD50) of 456.4 mg/kg. The protective index (PI = TD50/ED50) for compound 4 m was 67.1, which was significantly higher than that for the reference drug carbamazepine (PI = 6.4).
authors.affiliation: College of Pharmacy, Yanbian University, Jilin, PR China.
authors.forename: Xian-Yu
authors.initials: XY
authors.lastname: Sun
authors.forename: Cheng-Xi
authors.initials: CX
authors.lastname: Wei
authors.forename: Xian-Qing
authors.initials: XQ
authors.lastname: Deng
authors.forename: Zhi-Gang
authors.initials: ZG
authors.lastname: Sun
authors.forename: Zhe-Shan
authors.initials: ZS
authors.lastname: Quan
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000627:therapeutic use*; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D051379:Mice; D010793:Phthalazines / Q000138:chemical synthesis / Q000627:therapeutic use*; D045442:Rotarod Performance Test; D012640:Seizures / Q000188:drug therapy*; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D010793:Phthalazines