6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity.
A series of 6-(substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines was prepared for pharmacological evaluation, and, because of an interesting chemical isomerization, a similar series of 4-(substituted-amino)-6H-s-triazolo[4,3-alpha][1,4]benzodiazepines was also obtained. Pharmacological evaluation of these compounds demonstrated that8-choloro-1-methyl-6-piperidino-4H-s-triazolo[4,3-a][1,4]benzodiazpin e (10) had interesting activity in tests useful for detecting antianxiety activity, while the corresponding 4-piperidino derivative (15) had little activity in these tests. A brief discussion of a possible mechanism for the isomerization is also included.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D007536:Isomerism; D008297:Male; D051379:Mice; D008958:Models, Molecular; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology
D014151:Anti-Anxiety Agents; D014230:Triazoles; D001569:Benzodiazepines