Studies on 1-substituted 4-(1,2-diphenylethyl)piperazine derivatives and their analgesic activities. 2. Structure-activity relationships of 1-cycloalkyl-4-(1,2-diphenylethyl)piperazines

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Abstract
Forty-six 1-cycloalkyl-4-(1,2-diphenylethyl)piperazines were synthesized. The influence of substituents on phenyl groups of 1-cycloalkyl-4-(1,2-diphenylethyl)piperazines 1-3 on the analgesic activity investigated in experimental animals. The most active compounds, 4-6, in this series had a m-hydroxyl group on the 2-phenyl group of 1-3, while morphine has a phenolic hydroxyl group para to the aminoethyl moiety. Their activities were 23-56 and 23-38 times those of their original compounds 1-3 and morphine, respectively, tested by the D''Amour-Smith method after s.c. administration [in rats and mice].