9-(2-fluorobenzyl)-6-(alkylamino)-9H-purines. A new class of anticonvulsant agents

Article abstract of DOI:10.1021/jm00400a019

Several substituted aryl and 6-alkylamino analogues of the anticonvulsant purine 9-(2-fluorobenzyl)-6-(methylamino)-9H-purine were synthesized and tested for anticonvulsant activity against maximal electroshock-induced seizures (MES) in rats. Derivatives with a second fluoro substituent in the 5- or 6-position of the aryl moiety were very active with ip ED₅₀'s that ranged from 2 to 4 mg/kg. Congeners in which the purine 6-substituent was varied among a number of alkylamino groups possessed potent activity against MES that was comparable to or several times better than phenytoin.