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

Author(s): Xia Huang, Tie Chen, Rong-Bi Han, Feng-Yu Piao*.

Journal Name: CNS & Neurological Disorders - Drug Targets

Volume 17 , Issue 6 , 2018

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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.

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Article Details

VOLUME: 17
ISSUE: 6
Year: 2018
Page: [448 - 457]
Pages: 10
DOI: 10.2174/1871527317666180704101332
Price: $58

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