Synthesis and pharmacological evaluation of 6,8-diaryl 1,2,4-triazolo [4,3,-b] and 1,2,3,4,-tetrazolo [1,5-b] pyridazines.
A series of 6,8-diaryl-1,2,4-triazolo[4,3-b] and 1,2,3,4-tetrazolo[1,5-b]pyridazines was synthesized from suitable chloropyridazines. The compounds were screened in mice for their ability to antagonize maximal electroshock-, pentylenetetrazole- and bicuculline-induced seizures; sedative effects were evaluated by a study of the spontaneous motor activity. Some of pyridazine derivatives exhibited appreciable anticonvulsant activity. Substituting the phenyl ring in the 6-position with an halogen atom led to a substantial increase of activity. Furthermore, none of the compounds was notably active in tests predictive of anxiolytic activity.
Rubat
C
C
Laboratoire de Chimie Therapeutique, Faculté de Pharmacie, Clermont-Ferrand, France.
Coudert
P
P
Couquelet
J M
JM
Tronche
P
P
Bastide
J
J
Bastide
P
P
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis*; D000927:Anticonvulsants / Q000138:chemical synthesis*; D001393:Azoles / Q000138:chemical synthesis*; D001522:Behavior, Animal / Q000187:drug effects; D001640:Bicuculline; D055598:Chemical Phenomena; D002621:Chemistry; D004597:Electroshock; D006993:Hypnotics and Sedatives; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010433:Pentylenetetrazole; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001393:Azoles; D006993:Hypnotics and Sedatives; D011724:Pyridazines; D013777:Tetrazoles; D014230:Triazoles; D010433:Pentylenetetrazole; D001640:Bicuculline