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SYNTHESIS, ANTICONVULSANT, BENZOTRIAZOLOAZEPINES

Abstract

Xia Huang, Rong-Bi Han, Feng-Yu Piao, Tie Chen

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 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 MES (ED50=26.4, PI =3.2) and against scPTZ (ED50=40.2, PI =2.1). Possible structure–activity relationship is discussed.

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