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.
MeSH terms
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Administration, Oral
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Animals
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Anticonvulsants / chemical synthesis*
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Anticonvulsants / pharmacokinetics
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Anticonvulsants / pharmacology
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Dose-Response Relationship, Drug
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Drug Design
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Naphthyridines / chemical synthesis*
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Naphthyridines / pharmacokinetics*
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Naphthyridines / pharmacology
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Rats
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Seizures / drug therapy
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Seizures / prevention & control
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Structure-Activity Relationship
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Tetrahydroisoquinolines
Substances
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Anticonvulsants
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Naphthyridines
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Tetrahydroisoquinolines