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

Bioorg Med Chem Lett. 2003 May 19;13(10):1627-9. doi: 10.1016/s0960-894x(03)00288-9.

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

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

Substances

  • Anticonvulsants
  • Naphthyridines
  • Tetrahydroisoquinolines