Evaluation of a series of anticonvulsant 1,2,3,4-tetrahydroisoquinolinyl-benzamides

Bioorg Med Chem. 2000 Aug;8(8):2085-94. doi: 10.1016/s0968-0896(00)00149-8.

Abstract

SAR studies around a series of N-(tetrahydroisoquinolinyl)-2-methoxybenzamides, identified by high-throughput screening at the novel SB-204269 binding site, have provided compounds such as 13, 29-33 with high affinity and excellent anticonvulsant activity in animal models.

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis
  • Anticonvulsants / chemistry*
  • Anticonvulsants / metabolism
  • Anticonvulsants / pharmacology*
  • Benzamides / chemical synthesis
  • Benzamides / chemistry*
  • Benzamides / metabolism
  • Benzamides / pharmacology*
  • Benzopyrans / metabolism
  • Binding Sites
  • Brain Chemistry
  • Drug Design*
  • Drug Evaluation, Preclinical
  • Isoquinolines / chemical synthesis
  • Isoquinolines / chemistry*
  • Isoquinolines / metabolism
  • Isoquinolines / pharmacology*
  • Male
  • Mice
  • Models, Molecular
  • Molecular Structure
  • Radioligand Assay
  • Rats
  • Seizures / drug therapy
  • Structure-Activity Relationship

Substances

  • Anticonvulsants
  • Benzamides
  • Benzopyrans
  • Isoquinolines
  • SB 204269