Synthesis and structure-affinity relationships at the central benzodiazepine receptor of pyridazino[4,3-b]indoles and indeno[1,2-c]pyridazines

Bioorg Med Chem. 1999 Aug;7(8):1533-8. doi: 10.1016/s0968-0896(99)00093-0.

Abstract

A series of 2-aryl-3-chloro-2H-pyridazino[4,3-b]indoles, 2-aryl-3-methoxy-2H-pyridazino[4,3-b]indoles, and 2-aryl-2,5-dihydroindeno[1,2-c]pyridazino-3(3H)-ones has been prepared and tested for their ability to inhibit the [3H]flunitrazepam binding to the central benzodiazepine receptor. SAR are presented and discussed in comparison with existing pharmacophore models.

MeSH terms

  • Hydrogen Bonding
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Pyridazines / chemical synthesis*
  • Pyridazines / chemistry
  • Pyridazines / pharmacology
  • Receptors, GABA-A / drug effects*
  • Structure-Activity Relationship

Substances

  • Indoles
  • Pyridazines
  • Receptors, GABA-A