Document Report Card

ID: ALA3244037

Journal: J Med Chem

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

Authors: Hester JB, Von Voigtlander P.

Abstract: 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.

CiteXplore: 42799

DOI: 10.1021/jm00197a021