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

Abstract
A series of 1-substituted 6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines was prepared and evaluated for CNS activity in mice. Electronegative substituents, such as trifluoromethyl, were detrimental to activity in this series but 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 analogs with 4-methyl-1-piperazinyl and 4-morpholinyl substituents at C-1 were of particular interest.