PMID: 42799Nov 1, 1979

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

Journal of Medicinal Chemistry
J B Hester, P Von Voigtlander

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.

Citations

Jun 28, 1992·Annals of the New York Academy of Sciences·M A VargasC B Nemeroff
Sep 22, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Ming BianZhe-Shan Quan
Jul 18, 2006·Bioorganic & Medicinal Chemistry·Hong-Guang JinZhe-Shan Quan
Mar 31, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lidija KosychovaŽilvinas Anusevičius
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