Pyrazolodiazepines. III. 4-Aryl-1,6,7,8-tetrahydro-1,3-dialkylpyrazolo[3,4-e][1,4]diazepines as antidepressant agents

Journal of Medicinal Chemistry
1981.0

Abstract

A series of 4-aryl-1,6,7,8-tetrahydro-1,3-dialkylpyrazolo[3,4-e][1,4]diazepines was prepared. The principal pharmacological property of these diazepines is the potentiation of certain behavior responses to methamphetamine in several animal models. Drug potentiation of the anorectic effects of methamphetamine in milk drinking (rats) became a standard primary screen (ME) for antidepressant activity in this laboratory, and a significant number of these new pyrazolodiazepines showed stronger effects than imipramine in this screen. One compound (3, zometapine) is being studied in the clinic as an antidepressant. These diazepines were obtained readily in moderate to good yield from the reaction of (1,3-dialkyl-5-chloro-1H-pyrazol-4-yl)arylmethanones (V) with 1,2 diamines.

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