Heteroaryl-substuted semicarbazones: Synthesis and anticonvulsant activity of N-(3-methylpyridin-2-yl)-substituted semicarbazones

✍ Scribed by Shalini Mehta; Roheeth Kumar Pavana; Perumal Yogeeswari; Dharmarajan Sriram; James Stables

• Publisher: Journal of Heterocyclic Chemistry
• Year: 2006
• Tongue: English
• Weight: 343 KB
• Volume: 43
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.5570430522

✦ Synopsis

A series of substituted N-(3-methylpyridin-2-yl) semicarbazones was designed and synthesized to meet the structural requirements essential for anticonvulsant activity. The structures of all the synthesized compounds were confirmed by means of spectral and elemental analysis. All the compounds were evaluated for their anticonvulsant activity by maximal electroshock seizures (MES) test, subcutaneous pentylenetetrazole (scPTZ) screen, subcutaneous strychnine (scSTY) pattern test and subcutaneous picrotoxin (scPIC) seizure threshold test along with the behavioral, and neurotoxicity evaluation. A number of N-(3-methylpyridin-2-yl) semicarbazone derivatives exhibited significant protection after intraperitoneal administration at the dose of 100 and 300 mg/kg. Compound N 1 -(3-methylpyridin-2-yl)-N 4 -(isatin) semicarbazone ( 19) emerged as the most active analogue of the series, being more effective in most of the test models than ethosuximide and sodium valporate.