Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
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.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis*; D000927:Anticonvulsants; D000959:Antihypertensive Agents / Q000138:chemical synthesis; D001667:Binding, Competitive; D055598:Chemical Phenomena; D002621:Chemistry; D003220:Conflict, Psychological; D003975:Diazepam / Q000378:metabolism; D008297:Male; D011724:Pyridazines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D000959:Antihypertensive Agents; D011724:Pyridazines; D014230:Triazoles; D003975:Diazepam