Journal of Medicinal Chemistry 1988-03-01

6-(Alkylamino)-9-benzyl-9H-purines. A new class of anticonvulsant agents.

J L Kelley, M P Krochmal, J A Linn, E W McLean, F E Soroko

Index: J. Med. Chem. 31(3) , 606-12, (1988)

Full Text: HTML

Abstract

Several 9-alkyl-6-substituted-purines were synthesized and tested for anticonvulsant activity against maximal electroshock-induced seizures (MES) in rats. Most compounds were prepared in three steps from 5-amino-4,6-dichloropyrimidine or in two steps via alkylation of 6-chloropurine. Potent anticonvulsant activity against MES resided in compounds that contain a benzyl substituent at the 9-position of 6-(methylamino)- or 6-(dimethyl-amino)purine. Among commonly used agents for control of seizures, this type of structure represents a new class of potent anticonvulsant agents.