The design of 8,8-Dimethyl[1,6]naphthyridines as potential anticonvulsant agents

Nigel E Austin,Michael S Hadley,John D Harling,Frank P Harrington,Gregor J Macdonald,Darren J Mitchell,Graham J Riley,Tania O Stean,Geoffrey Stemp,Sharon C Stratton,Mervyn Thompson,Neil Upton

Bioorganic & Medicinal Chemistry Letters（2003）

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摘要

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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