SYNTHESIS, ANTICONVULSANT, BENZOTRIAZOLOAZEPINES

  • Xia Huang Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, People’s Republic of China
  • Rong-Bi Han Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, People’s Republic of China
  • Feng-Yu Piao Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, People’s Republic of China
  • Tie Chen Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, People’s Republic of China

Abstract

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.

Published
May 24, 2017
How to Cite
HUANG, Xia et al. SYNTHESIS, ANTICONVULSANT, BENZOTRIAZOLOAZEPINES. International Journal of Drug Research and Technology, [S.l.], v. 7, n. 2, p. 4, may 2017. ISSN 2277-1506. Available at: <http://ijdrt.com/index.php/drug-research-and-technology/article/view/synthesis-anticonvulsant-benzotriazoloazepines>. Date accessed: 14 aug. 2018.
Section
Research Article