Details

Autor(en) / Beteiligte

• Hester, Jackson B
• VonVoigtlander, Philip
• Evenson, Gerald N

Titel

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

Ist Teil von

• Journal of medicinal chemistry, 1980-08, Vol.23 (8), p.873-877

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

1980

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.