Details

Autor(en) / Beteiligte

• Hester, Jackson B
• Von Voigtlander, Philip

Titel

6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity

Ist Teil von

• Journal of medicinal chemistry, 1979-11, Vol.22 (11), p.1390-1398

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

1979

Quelle

MEDLINE

Beschreibungen/Notizen

• A series of 1-substituted 6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines was prepared and evaluated for central nervous system activity. It was found that electronegative substituents, such as trifluoromethyl, were detrimental to activity in this series. On the other hand, many compounds with electron-donating substituents at C-1 had interesting activity. In addition to showing anxiolytic potential, some were also active in tests useful for detecting antidepressant and antipsychotic activity. Several analogues with 4-methyl-1-piperazinyl and 4-morpholinyl substituents at C-1 were of particular interest.