Anticonvulsant screening of three N-(2,6-dimethylphenyl)- substituted-benzamides

  • EO Afolabi
  • VI Okolie
Keywords: Anticonvulsant, Benzamide, Epilepsy and Seizures

Abstract

The N-(substituted)-4-aminobenzamides have provided several anticonvulsants that have been extensively investigated. In these series, Ameltolide®, 4-amino-N-(2,6-dimethylphenyl) benzamide (LY201116) is the most potent analogue studied to date. This drug is inactivated in vivo by metabolic N-acetylation, resulting in 4-(acetylamino)-N-(2,6-dimethylphenyl)benzamide. Efforts to limit this metabolic inactivation led to the synthesis of two analogues: 3,4-diamino-N-(2,6-dimethylphenyl) benzamide and N-(2,6-dimethylphenyl) benzamide. The anticonvulsant activities of these two compounds were determined against their ability to inhibit pentylenetetrazole induced seizure in rats after oral administration at three dose levels, i.e. 10mg/Kg, 30mg/Kg, and 100mg/Kg at 30
minutes interval. In addition, the effect of time of oral administration at 30mg/Kg dose level was determined at time intervals of 1h, 2h, and 4h respectively for 3,4-diamino-N-(2,6-dimethylphenyl)benzamide. Our results were compared with that of ameltolide® and carbamazepine.

Keywords: Anticonvulsant, Benzamide, Epilepsy and Seizures

Published
2013-02-12
Section
Articles

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eISSN: 0189-8442