title: 9-(2-Fluorobenzyl)-6-(alkylamino)-9H-purines. A new class of anticonvulsant agents.
abstract: Several substituted aryl and 6-alkylamino analogues of the anticonvulsant purine 9-(2-fluorobenzyl)-6-(methyl-amino)-9H-purine (1) 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.
authors: Organic Chemistry Department, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709.
authors: J L
authors: JL
authors: Kelley
authors: M P
authors: MP
authors: Krochmal
authors: J A
authors: JA
authors: Linn
authors: E W
authors: EW
authors: McLean
authors: F E
authors: FE
authors: Soroko
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D001593:Benzyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D001593:Benzyl Compounds; D011687:Purines