Microwave synthesis and anticonvulsant activity of 2-benzyl-1(2H)-phthalazinones

✍ Scribed by Milton J. Kornet; George Shackleford

• Publisher: Journal of Heterocyclic Chemistry
• Year: 1999
• Tongue: English
• Weight: 136 KB
• Volume: 36
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.5570360444

✦ Synopsis

Abstract

Microwave irradiation of 1(2__H__)‐phthalazinone with benzyl halides and potassium carbonate in dimethyl‐formamide afforded 2‐benzyl‐1(2__H__)phthalazinones in modest yields. These products were tested in mice and rats in maximal electroshock and pentylenetetrazole seizure models for anticonvulsant activity, and in the rotorod test for neurotoxicity. A majority of the compounds exhibited anticonvulsant protection. The p‐aminobenzyl analog 1f was the most active compound in the maximal electroshock assay; it's ED~50~ value was 19.46 mg/kg and the TD~50~ was 61.35 mg/kg. In the rat, the values were 3.71 mg/kg and >125 mg/kg, respectively.