Abstract

Synthesis and biological evaluation of some newer 1,5-benzodiazepine derivatives as potential anticonvulsant agents

Benzodiazepines and their derivatives were reported to have wide biological activities and were synthesized by the reaction between substituted benzaldehydes and substituted ketones in presence of sodium hydroxide to afford chalcones and further reaction between 1,2-diamine under condensation with chalcones in the presence of glacial acetic acid to afford substituted 1,5-benzodiazepines (1b-10b) in good yield and further methylation with methyl iodide in basic medium gave 2,4-Disubstituted phenyl-1-methyl-1H-benzodiazepines (1c-10c) and on acetylation with acetyl chloride in basic medium yielded 2,4-Disubstituted phenyl-1-acetyl-1H-benzodiazepines (1d-5d). The chemical structures of the newly synthesized compounds have been confirmed by IR, 1H-NMR, MASS spectral data and elemental analysis. All the newly synthesized compounds were evaluated for anticonvulsant activities and their neurotoxicity studies by maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (ScPTZ) and rotorod test respectively, of which compounds 1c, 3c, 6c, 8c and 9c exhibited potent anticonvulsant results and in the neurotoxicity screening, most of the compounds were devoid of toxicity at the dose of 100 and 300mg/kg.
Author(s): Jyoti, Mithlesh Yadav and Devender Pathak

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