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.