title: Synthesis and anticonvulsant and antidepressant activity of 2-(5-bromo-2,3-dioxoindolin)-N-substituted phenylacetamide derivatives.
abstract: 16 2-(5-bromo-2,3-dioxoindolin-1-yl)-N-substituted phenylacetamide derivatives were synthesized. The chemical structures of the compounds were proved by IR, 1H-NMR, 13C-NMR, Mass spectrometric data and microanalyses. The antidepressant activities of the compounds were investigated by Porsolt's behavioural despair (the forced swimming test) in mice. 2-(5-bromo-2,3-dioxoi-ndolin-1-yl)-N-(2-fluorophenyl)acetamide(4f), 2-(5-bromo-2,3-dioxoindolin-1-yl)-N-(3-chlorophenyl)acetamide(4j), 2-(5-bromo-2,3-dioxoindolin-1-yl)-N-(4-bromophenyl)acetamide(4m) reduced 54.9-44.6% duration of immobility times at 100 mg · kg-1 dose level. Anticonvulsant activities were determined by substances pentylenetetrazloe(metrazol)(anti-PTZ) test, and neurotoxicities were determined by the rotarod toxicity test in mice. 12 synthesized compounds were found protective against PTZ at 100 mg ∙ kg-1 dose level.
authors.affiliation: School of Food, Drug & Medicine Zhejiang Ocean University, Zhoushan, P. R. China.
authors.forename: C
authors.initials: C
authors.lastname: Xie
authors.affiliation: School of Food, Drug & Medicine Zhejiang Ocean University, Zhoushan, P. R. China.
authors.forename: L-M
authors.initials: LM
authors.lastname: Tang
authors.affiliation: School of Food, Drug & Medicine Zhejiang Ocean University, Zhoushan, P. R. China.
authors.forename: C-Y
authors.initials: CY
authors.lastname: Pan
authors.affiliation: School of Food, Drug & Medicine Zhejiang Ocean University, Zhoushan, P. R. China.
authors.forename: L-P
authors.initials: LP
authors.lastname: Guan
mesh_terms: D000083:Acetanilides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003863:Depression / Q000188:drug therapy; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D008807:Mice, Inbred BALB C; D012640:Seizures / Q000188:drug therapy; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D018675:Toxicity Tests / Q000379:methods
chemical_list: D000083:Acetanilides; D000927:Anticonvulsants; D000928:Antidepressive Agents