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Synthesis and Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives

[ Vol. 17 , Issue. 6 ]

Author(s):

Xia Huang, Tie Chen, Rong-Bi Han and Feng-Yu Piao*   Pages 448 - 457 ( 10 )

Abstract:


Background & Objective: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1).

Conclusion: Possible structure-activity relationship was discussed.

Keywords:

Anticonvulsant activity, toxicity, benzotriazoloazepine, synthesis, pharmacological, maximal electroshock test.

Affiliation:

Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province

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