Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines

J Med Chem. 1981 May;24(5):592-600. doi: 10.1021/jm00137a020.


The synthesis of a series of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines (VIII) is reported. Some of these derivatives show activity in tests predictive of anxiolytic activity [(a) protection against pentylenetetrazole-induced convulsions; (b) thirsty rat conflict procedure]. They also represent a new class of compound which inhibits [3H]diazepam binding. Structure--activity correlations, as well as the ability of structures VIII to inhibit [3H]diazepam binding (in vitro), are discussed.

MeSH terms

  • Animals
  • Anti-Anxiety Agents / chemical synthesis*
  • Anticonvulsants
  • Antihypertensive Agents / chemical synthesis
  • Binding, Competitive
  • Chemical Phenomena
  • Chemistry
  • Conflict, Psychological
  • Diazepam / metabolism
  • Male
  • Pyridazines / chemical synthesis
  • Pyridazines / pharmacology
  • Rats
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology


  • Anti-Anxiety Agents
  • Anticonvulsants
  • Antihypertensive Agents
  • Pyridazines
  • Triazoles
  • Diazepam