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The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents
Authors:Austin Nigel E  Hadley Michael S  Harling John D  Harrington Frank P  Macdonald Gregor J  Mitchell Darren J  Riley Graham J  Stean Tania O  Stemp Geoffrey  Stratton Sharon C  Thompson Mervyn  Upton Neil
Affiliation:Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline Research & Development Limited, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
Abstract:Starting from a series of 7-linked tetrahydroisoquinoline derivatives, as exemplified by SB-270664, a new series of 8,8-dimethylnaphthyridine compounds has been identified. SAR studies around these attractive leads have provided compounds such as 12 which display excellent anticonvulsant activity and an encouraging pharmacokinetic profile in vivo.
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