title: Synthesis and anticonvulsant activity of ethyl 2,2-dimethyl-1-(2-substitutedhydrazinecarboxamido) cyclopropanecarboxylate derivatives.
abstract: In this study on the development of new anticonvulsants, fourteen ethyl 2,2-dimethyl-1-(2-substitutedhydrazinecarboxamido) cyclopropanecarboxylate derivatives were synthesized and tested for anticonvulsant activity using the maximal electroshock, subcutaneous pentylenetetrazole screens, which are the most widely employed seizure models for early identification of candidate anticonvulsants. Their neurotoxicity was determined applying the rotorod test. Two compounds 6f and 6k showed promising anticonvulsant activities in both models employed for anticonvulsant evaluation. The most active compound 6k showed the maximal electroshock-induced seizures with ED50 value of 9.2 mg/kg and TD50 value of 387.5 mg/kg after intraperitoneally injection to mice, which provided compound 6k with a protective index (TD50/ED50 ) of 42.1 in the maximal electroshock test.
authors.affiliation: Wuhan Economic and Technological Development Zone, School of Chemical and Environmental Engineering, Jianghan University, Wuhan, 430056, China.
authors.forename: Min
authors.initials: M
authors.lastname: Zhong
authors.forename: Yongmin
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xianran
authors.initials: X
authors.lastname: He
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D003521:Cyclopropanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D004597:Electroshock; D008297:Male; D051379:Mice; D045442:Rotarod Performance Test; D012640:Seizures / Q000188:drug therapy*
chemical_list: D000927:Anticonvulsants; D003521:Cyclopropanes; C015766:cyclopropanecarboxylic acid
keywords: Ethyl 2,2-dimethyl-1-(2-substitutedhydrazinecarboxamido) cyclopropanecarboxylate; MES test; anticonvulsant activity; scPTZ test