1. The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents.
- Author
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Austin NE, Hadley MS, Harling JD, Harrington FP, Macdonald GJ, Mitchell DJ, Riley GJ, Stean TO, Stemp G, Stratton SC, Thompson M, and Upton N
- Subjects
- Administration, Oral, Animals, Anticonvulsants pharmacokinetics, Anticonvulsants pharmacology, Dose-Response Relationship, Drug, Drug Design, Naphthyridines pharmacology, Rats, Seizures drug therapy, Seizures prevention & control, Structure-Activity Relationship, Tetrahydroisoquinolines, Anticonvulsants chemical synthesis, Naphthyridines chemical synthesis, Naphthyridines pharmacokinetics
- 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.
- Published
- 2003
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