Pyrazolodiazepines. 1,3 (and 2,3) dialkyl 4,6 dihydro 8 arylpyrazolo[4,3 e][1,4] diazepin 5 ones as antianxiety agents

Article abstract of DOI:10.1021/jm00270a007

A series of 1, 3 (and 2, 3) dialkyl 4, 6 dihydro 8 arylpyrazolo [4, 3 e][1, 4] diazepin 5 ones was synthesized and evaluated for psychotropic activity. Intermediates are new dialkylnitropyrazolyl aryl ketones prepared from dialkylnitropyrazolecarboxylic acids. Many of these pyrazolodiazepines exhibit high CNS activity in animals. One compound, 1 ethyl 4, 6 dihydro 3 methyl 8 phenylpyrazolo [4, 3 e] [1, 4] diazepin 5 (1H) one is about as potent as diazepam as an antianxiety agent with less sedative properties and is being studied in the clinic.