Synthesis and pharmacological evaluation of newer substituted benzoxazepine derivatives as potent anticonvulsant agents

Abstract

A series of 2-substitutedphenyl-3-(substitutedphenylamino)methyl-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (4a–4p) and 2-substitutedphenyl-3-substitutedphenylazo-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (5a–5p) have been synthesized from 2-substitutedphenyl-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (3a–3d) by the Mannich reaction and diazotization reaction, respectively. All these compounds were screened, in vivo, for their anticonvulsant activity and acute toxicity studies. Compounds 4p and 5p were found to be most potent compounds of this series and were compared with the reference drug phenytion sodium, lamotrigine and sodium valproate. The structures of these compounds have been established by IR, 1H NMR and mass spectroscopic data.